z-isomer

Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.

Eltanexor Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC50s of 100 nM-50 μM, < 100 nM, > 30 μM, respectively.Eltanexor Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.

Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.

Tamoxifen is an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM).

Endoxifen E-isomer (E-Endoxifen) is the E-isomer of (Z)-Endoxifen. Endoxifen E-isomer has antiestrogenic effects.

Damascenone is a mixture of E- and Z-isomer damascenones, characteristic compounds with anti-inflammatory properties derived from Epipremnum pinnatum.

(Z)-JIB-04 (NSC 693627) is an isomer of JIB-04.

12(Z),15(Z)-Heneicosadienoic acid, an ω-6 very long-chain polyunsaturated fatty acid, serves as a positional isomer of heneicosadienoic acid, which is scarcely found in living organisms.

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob/obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

(Z)-Aconitic acid is the cis-isomer of Aconitic acid.is an intermediate in the tricarboxylic acid cycle produced by the dehydration of citric acid.

(E)-4-Hydroxytamoxifen is a less active isomer of (Z)-4-hydroxytamoxifen and also is an estrogen receptor modulator.

9(Z),11(Z)-Octadecadienoic acid, an isomer of linoleic acid, demonstrates antitumor activity with an EC50 value of 446.1 µM [1].

8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland microsomes (IC50= 31 μM).4 1.Crombie, L., and Holloway, S.J.The biosynthesis of calendic acid, octadeca-(8E,10E, 12Z)-trienoic, acid, by developing marigold seeds: origins of (E,E,Z) and (Z,E,Z) conjugated triene acids in higher plantsJ. Chem. Soc. Perk. T. 12425-2434(1985) 2.Yasui, Y., Hosokawa, M., Kohno, H., et al.Growth inhibition and apoptosis induction by all-trans-conjugated linolenic acids on human colon cancer cellsAnticancer Res.26(3A)1855-1860(2006) 3.Shinohara, N., Ito, J., Tsuduki, T., et al.Jacaric acid, a linolenic acid isomer with a conjugated triene system, reduces stearoyl-CoA desaturase expression in liver of miceJ. Oleo Sci.61(8)433-441(2012) 4.Nugteren, D.H., and Christ-Hazelhof, E.Naturally occurring conjugated octadecatrienoic acids are strong inhibitors of prostaglandin biosynthesisProstaglandins33(3)403-417(1987)

Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride), a tamoxifen metabolite, is an effective and specific Estrogen Response Modifier (SERM).

Prostaglandin D2 (PGD2) is one of the five principal prostaglandins enzymatically derived from PGH2. It is abundantly generated in the cerebrospinal fluid (CSF) by lipocalin-type PGD synthase and in peripheral regions by myeloid cells, such as mast cells and basophils, via leukocyte-type PGD synthase. The compound 1,25-trans-PGD2 is an isomer of PGD2, characterized by the alteration of the double bond between carbons 5 and 6 from cis(Z) to trans(E). This trans isomer, found as a 2-5% impurity in most commercial PGD2 bulk drug preparations, is primarily synthesized as an analytical standard to identify and quantify this impurity. Based on existing studies of trans isomers of F-type prostaglandins, 5-trans-PGD2 likely exhibits biological activity comparable to its cis isomer, although no specific published reports confirm this for 5-trans-PGD2.

(Z)-4EGI-1, the Z-isomer of 4EGI-1, serves as an inhibitor of both the eIF4E/eIF4G interaction and translation initiation. It effectively binds to eIF4E, exhibiting an IC50 of 43.5 μM and a Kd value of 8.74 μM. Notably, (Z)-4EGI-1 possesses anticancer activity[1][2].

(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor that preferentially inhibits the TK activity of the EGF receptor, restricting the EGF-stimulated growth of cultured cells. It demonstrates an IC50 of 11 μM for DNA synthesis in HN5 cells, showcasing thrice the potency of its isomer, (E)-RG-13022 (IC50 = 38 μM). This compound is applied in breast cancer cell research [1] [2].

Z-2-Octenoic acid, the Z-isomer of 2-Octenoic acid, is also known as trans-2-Octenoic acid and serves as a metabolite in Mucor species.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on reducing intraocular pressure in particular, of 5-trans latanoprost.

Latanoprost is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. 5-trans Latanoprost is an isomer of latanoprost wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity of between 2-5% in most commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, 5-trans latanoprost's biological activity is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on the intraocular hypotensive activity in particular, of 5-trans latanoprost.

(Z)-MDL 105519 is an inactive isomer of MDL105519.

(±)8-HEPE is produced by the non-enzymatic oxidation of EPA, containing equal amounts of 8(S)-HEPE and 8(R)-HEPE. The ability of (±)8-HEPE to induce hatching of E. modestus and B. balanoides eggs is probably due to the presence of the 8(R) isomer within the racemic mixture.[1][2]

(Z)-Pitavastatin calcium is the Z-isomer of Pitavastatin hemicacium and a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase.

9(Z),11(E),13(Z)-Octadecatrienoic acid methyl ester, an isomer of 9(Z),11(E),13(E)-octadecatrienoic acid methyl ester and the methyl ester derivative of 9(Z),11(E),13(Z)-octadecatrienoic acid, serves as a standard for quantifying 9(Z),11(E),13(Z)-octadecatrienoic acid in wild growing pomegranate (P. granatum) seed oil [Matreya, LLC. Catalog No. 1240].

Z-CITCO acts as an agonist for the constitutive androstane receptor (CAR; with an EC50 of 3.9 µM in human receptor reporter assays) and is the cis isomer of the CAR agonist CITCO.

Z-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene is the fluorine analog of Methyl eugenol (ME), the attractant of the oriental fruit fly B. dorsalis.The E-isomer is twice as active as the Z-isomer Z-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene.

(Z)-Capsaicin (Zucapsaicin) is a medication used to treat osteoarthritis of the knee and Others neuropathic pain.(Z)-Capsaicin is a synthetic cis isomer of natural capsaicin that has shown therapeutic efficacy in pain accompanying osteoarthritis of the knee.

R 80123 is a highly selective inhibitor of phosphodiesterase,is the Z-isomer of R 79595