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third-generation

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  • Inhibitors & Agonists
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Osimertinib
AZD-9291,Mereletinib
T24901421373-65-0
Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
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CCT367766
T149082229856-58-8In house
CCT367766 is a potent, PROTAC-based, third-generation, iso-functional pirin-targeted protein degradation probe (PDP) that depletes pirin expression at low concentrations.CCT367766 has an IC50 value of 490 nM for the CRBN-DDB1 complex.CCT367766 has a good affinity for recombinant pirin and CRBN. CCT367766 has a good affinity for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. cct367766 is a potent orally active protein that reduces the expression of pirin at low concentrations.
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Levofloxacin hydrochloride
T8747177325-13-2
Levofloxacin is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Levofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth.
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Osimertinib mesylate
Mereletinib mesylate,AZD-9291 mesylate
T36341421373-66-1
Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
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TargetMol | Citations Cited
Cefditoren pivoxil
ME 1207,Cefditoren pivaloyloxymethyl ester,Cefditoren pivoxyl
T1405117467-28-4
Cefditoren pivoxil (ME 1207) is a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity.
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Ceftriaxone sodium hydrate
Ceftriaxone Sodium Trihydrate,Ceftriaxone disodium hemiheptahydrate,Ceftriaxone sodium
T1223104376-79-6
Ceftriaxone sodium hydrate is a broad-spectrum cephalosporin antibiotic with a very long half-life and high penetrability to meninges, eyes and inner ears.
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Ceftiofur sodium
Naxcel,Sodium ceftiofur
T0198104010-37-9
Ceftiofur sodium (Naxcel), an antibiotic of the cephalosporin type (third generation), is used as veterinary medicine.
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Levofloxacin hydrate
Levaquin hydrate,Cravit hydrate,Quixin hydrate,Levofloxacin Hemihydrate,Tavanic hydrate,Iquix hydrate
T1451138199-71-0
Levofloxacin hydrate (Cravit hydrate) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Levofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth.
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Ceftibuten dihydrate
Sch-39720 dihydrate
T4405118081-34-8
Ceftibuten dihydrate (Sch-39720 dihydrate) is the dihydrate form of ceftibuten, and is a third-generation cephalosporin with antibacterial activity.
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Cefpodoxime proxetil
T499887239-81-4
Cefpodoxime is an oral third generation cephalosporin antibiotic. It is active against most Gram positive and Gram negative bacteria. It is commonly used to treat acute otitis media, pharyngitis, and sinusitis. Cefpodoxime proxetil is a prodrug which is a
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Levocetirizine Dihydrochloride
Xyzal Dihydrochloride,(-)-Cetirizine Dihydrochloride
T22354130018-87-0
Levocetirizine Dihydrochloride (Xyzal Dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Acting as an antihistaminic agent, it specifically targets the histamine H1-receptor. Levocetirizine Dihydrochloride is the R-enantiomer of Cetirizine, which gives it a higher affinity for the H1-receptor than the S-enantiomer. Due to this enhanced affinity, Levocetirizine Dihydrochloride is effective in treating allergic rhinitis and chronic idiopathic urticaria.
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7-10 days
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Glimepiride
Glimperide,HOE-490
T012793479-97-1
Glimepiride (HOE-490) is a long-acting, third-generation sulfonylurea with hypoglycemic activity.
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Cefotiam hydrochloride
Pansporin,SCE-963 hydrochloride,Pansporine,Cefotiam dihydrochloride,Halospor
T161666309-69-1
Cefotiam hydrochloride (SCE-963 hydrochloride) is the hydrochloride salt form of cefotiam, a third-generation, semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity. Cefotiam binds to penicillin-binding proteins (PBPs), transpeptidases that are responsible for crosslinking of peptidoglycan. By preventing crosslinking of peptidoglycan, cell wall integrity is lost and cell wall synthesis is halted.
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Cefotaxime sodium
Cefotaxim sodium salt,Cefotaxime sodium salt,Cefotaxim (sodium salt),HR-756 (sodium salt)
T091164485-93-4
Cefotaxime is a third-generation cephalosporin antibiotic. Like other third-generation cephalosporins, it has broad spectrum activity against Gram positive and Gram negative bacteria. In most cases, it is considered to be equivalent to ceftriaxone in terms of safety and efficacy. Cefotaxime sodium (Cefotaxim sodium salt) is marketed under various trade names including Claforan (Sanofi-Aventis).
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Cefpiramide acid
Cefpiramidum,Cefpiramido
T013870797-11-4
Cefpiramide acid (Cefpiramidum) is a third-generation cephalosporin antibiotic.
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Cefetamet pivoxil hydrochloride
Ro 15-8075
T7120111696-23-2
Cefetamet pivoxil hydrochloride (Ro 15-8075) is a third generation cephalosporin antibiotic with oral activity.
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Ceftiofur hydrochloride
Ceftiofur HCl,U-67279A,Excenel hydrochloride
T6268103980-44-5
Ceftiofur hydrochloride (U-67279A) is the hydrochloride salt form of ceftiofur, a semisynthetic, beta-lactamase-stable, broad-spectrum, third-generation cephalosporin with antibacterial activity.
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Cefixime
FK-027,Cefspan,Cefiximum,Cephoral,FR-17027,CL-284635
T093279350-37-1
Cefixime (FR-17027) is a broad-spectrum, third-generation cephalosporin antibiotic derived semisynthetically from the marine fungus Cephalosporium acremonium with antibacterial activity. As does penicillin, the beta-lactam antibiotic cefixime inhibits bacterial cell wall synthesis by disrupting peptidoglycan synthesis, resulting in a reduction in bacterial cell wall stability and bacterial cell lysis. Stable in the presence of a variety of beta-lactamases, this agent is more active against gram-negative bacteria and less active against gram-positive bacteria compared to second-generation cephalosporins.
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Cefodizime Sodium
T812686329-79-5
Cefodizime Sodium is a third generation cephalosporin antibiotic, has broad-spectrum activity
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Cefdinir
FK-482,CI-983,PD 134393
T013391832-40-5
Cefdinir (FK-482) is a third-generation, semi-synthetic cephalosporin antibiotic effective against common bacterial infections of the ear, sinus, throat, and skin.
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Ibandronic acid
Bonviva,Bondronat,Boniva
T1599114084-78-5
Ibandronic acid (Bonviva) is a third-generation amino-bisphosphonate with anti-resorptive and anti-hypercalcemic activities.
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4-6 weeks
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Laniquidar
T64133197509-46-9In house
Laniquidar (R101933) is a third generation non-competitive inhibitor of P-glycoprotein (P-gp) (IC50: 0.51 μM) with limited oral bioavailability. It can also be used to modulate multidrug resistance transporters.
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6-8 weeks
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simotaxel
T67809791635-59-1In house
Simotaxel is a semi-synthetic, orally bioavailable, third-generation taxane derivative and microtubule-stabilizing agent, with potential antineoplastic activity.
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Lorlatinib
PF-6463922,PF-06463922,Loratinib
T30611454846-35-5
Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
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Cefcapene pivoxil hydrochloride hydrate
Cefcapene Pivoxil Hydrochloride
T4990147816-24-8
Cefcapene pivoxil hydrochloride hydrate is the pivalate ester prodrug form of cefcapene, a semi-synthetic third-generation cephalosporin with antibacterial activity. After oral administration of cefcapene pivoxil, the ester bond is cleaved, releasing active cefcapene.
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Lasofoxifene Tartrate
CP-336156
T7839190791-29-8
Lasofoxifene Tartrate (CP-336156) is a third-generation, non-steroidal selective estrogen receptor modulator.
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Almonertinib mesylate
T98652134096-06-1
Almonertinib mesylate is an irreversible inhibitor of EGFR tyrosine kinase with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate can be used in the non-small cell lung cancer studies.
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E 4441
E-4441,E4441
T31590124668-12-8
E 4441 is a third-generation difluoroquinolone, which has good activity against G(+) aerobic bacteria and anaerobic bacteria in vitro and in vivo.
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6-8 weeks
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Sumarotene
Ro14-9706,Ro-14-9706,Ro 14-9706
T26238105687-93-2
Sumarotene, a third-generation retinoid, is used as a topical dermatologic agent for the repair of antikeratinization, photodamage, and antiproliferation.
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6-8 weeks
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Abivertinib HCl
T704461557268-90-2
Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. Abivertinib may be a promising novel agent for AML, with potential for combination treatment with HHT.
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6-8 weeks
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Cefditoren Pivoxil HCl
T706211448435-17-3
Cefditoren Pivoxil is a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity. Cefditoren pivoxil is a prodrug that is rapidly hydrolyzed by intestinal esterases during absorption to the microbiologically active cefditoren, an active aminothiazolyl cephalosporin. Cefditoren inactivates penicillin binding proteins (PBPs) thereby interfering with peptidoglycan synthesis and inhibiting bacterial cell wall synthesis.
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1-2 weeks
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Pradofloxacin
T81412195532-12-8
Pradofloxacin is a third-generation fluoroquinolone antibacterial agent.
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8-10 weeks
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Ro 14-1761
Ro-14-1761
T3434882502-19-0
Ro 14-1761 is a new third-generation cephalosporin.
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Cefotiam Hexetil Hydrochloride
T502495789-30-3
Cefotiam Hexetil Hydrochloride is a third-generation, semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity.
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SRS16-86
T90731793052-96-6
SRS16-86 is a novel third-generation ferrostatin, is an inhibitor of ferroptosis.
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Cefpodoxime proxetil-d3
TMID-0290
Cefpodoxime proxetil-d3 is a deuterated compound of Cefpodoxime proxetil. Cefpodoxime proxetil has a CAS number of 87239-81-4. Cefpodoxime is an oral third generation cephalosporin antibiotic. It is active against most Gram positive and Gram negative bacteria. It is commonly used to treat acute otitis media, pharyngitis, and sinusitis. Cefpodoxime proxetil is a prodrug which is absorbed and de-esterified by the intestinal mucosa to Cefpodoxime.
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35 days
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Cefpodoxime sodium
R3746,R 3763,R 3746,R-3746,R-3763
T4998L282619-04-3
Cefpodoxime sodium is a third generation cephalosporin antibiotic agent. It targets gram-positive and gram-negative bacteria, especially those responsible for otitis media and pharyngitis.
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3-Desacetyl Cefotaxime lactone
T1403066340-33-8
3-Desacetyl Cefotaxime lactone, the active metabolite of Cefotaxime, is derived from its sodium salt form, which is recognized as a third-generation cephalosporin antibiotic.
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7-10 days
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Zifanocycline
T741441420294-56-9
Zifanocycline (KBP-7072), a third-generation semisynthetic aminomethylcycline antibiotic, inhibits bacterial ribosome function, displaying broad-spectrum antibacterial activity in vitro against both Gram-positive and Gram-negative bacteria, notably multidrug-resistant strains. It is formulated for oral and injectable use, targeting research on acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections [1] [2].
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Ceftibuten
Sch 39720
T1075397519-39-6
Ceftibuten is a third-generation cephalosporin antibiotic.
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DAD
T62770
DAD is an ion channel blocker (blocks voltage-gated potassium channels) and is a third generation photoelectric switch that responds to visible light.
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10-14 weeks
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Iso-Fludelone
T68860691868-19-6
Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
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6-8 weeks
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Cefcanel free acid
T6926641952-52-7
Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg/ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
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6-8 weeks
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Finerenone-d5
TMIH-0235
Finerenone-d5 is a deuterated compound of Finerenone. Finerenone has a CAS number of 1050477-31-0. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). 
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7-10 days
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Marbofloxacin hydrochloride
T72175115551-26-3
Marbofloxacin hydrochloride, a third-generation fluoroquinolone and orally active antimicrobial agent, exhibits broad-spectrum bactericidal activity and high efficacy. It is utilized in the research of infections caused by both Gram-positive and Gram-negative bacteria, as well as Mycoplasma.
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1-2 weeks
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Cefpodoxime (free acid)
T4998L80210-62-4
Cefpodoxime (free acid) is an oral, third-generation cephalosporin antibiotic. It is active against most Gram-positive and Gram-negative organisms, except Pseudomonas aeruginosa, Enterococcus, and Bacteroides fragilis.
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Trilexium
TRX-E-009-1
T875651983180-82-0
Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].
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Inquiry
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(Rac)-Finerenone
(Rac)-Finerenone,(Rac)-BAY 94-8862
T384481050477-27-4
Rac-Finerenone, also known as (Rac)-BAY 94-8862, is the racemate derivative of Finerenone, a selective third-generation nonsteroidal mineralocorticoid receptor antagonist (MR) that is taken orally. With an IC50 value of 18 nM, Finerenone exhibits exceptional selectivity against the glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).
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Cefodizime
T1492269739-16-8
Cefodizime is a new cephalosporin antibiotic with a wide range of biological activities.Cefodizime is non-toxic to the kidneys and is well tolerated with immunomodulatory activity.Cefodizime has antimicrobial activity and is used in the study of serious infections of the respiratory and urinary systems.
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7-10 days
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