anti-fibrotic

Malotilate (Kantec) is a medicine used for the therapy of liver cirrhosis.

Apamin acetate (Apamine acetate) is a selective Ca2+-activated blocker of K+ (SK) channels, an 18-amino acid peptide neurotoxin found in bee toxins.Apamin acetate enhances synapse growth and regeneration following laceration injury to cortical neurons.Apamin acetate has anti-inflammatory and anti-fibrotic effects.

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

Aucubin (Rhinanthin) is an iridoid glycoside with anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.

24-Norursodeoxycholic acid (nor-UDCA) is a side chain-shortened C23 homolog of UDCA.It has shown potent anti-inflammatory, anti-cholestatic, and anti-fibrotic properties.It is a Ursodeoxycholic Acid derivative. It is superior to Ursodeoxycholic acid in the treatment of sclerosing cholangitis in Mdr2 (Abcb4) knockout mice

Mogroside III-E, a cucurbitane-type compound isolated from Siraitia grosvenorii, exhibits anti-inflammatory activity by attenuating LPS-induced acute lung injury in mice through the regulation of the TLR4 MAPK NF-κB axis via AMPK activation. Additionally, it demonstrates anti-fibrotic activity by reducing pulmonary fibrosis through Toll-Like receptor 4 pathways.

Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50 Ki: 60 41 nM).

Naproxcinod, a nitric oxide-releasing NSAID derivative, significantly improved skeletal muscle strength and fatigue resistance in sedentary and exercise mice, reducing inflammatory infiltration and fibrotic deposition in the myocardium and diaphragm. In a

FT011, a direct anti-fibrotic agent,attenuates cardiac remodelling and dysfunction in experimental diabetic cardiomyopathy.

MnTBAP chloride (Mn(III)TBAP) is a cell-permeable superoxide dismutase (SOD) mimetic and peroxynitrite scavenger that reduces the doubling time of SOD-E. coli by a factor of 2. MnTBAP chloride exhibits anti-inflammatory effects through upregulation of BMPR-II and inhibition of NFκB signaling. mnTBAP chloride is a manganese porphyrin complex with antioxidant properties and has potential for use in the study of fibrotic responses in chronic kidney diseases (CKDs).

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual-target PROTAC capable of directing ubiquitination and degradation of Smad3 while also elevating HIF-α protein levels, exhibiting multipath anti-fibrotic and renal protective functions, making it valuable for renal anemia research [1].

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom) that selectively blocks Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity. This component of bee venom is strongly basic in nature.

VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.

Halofuginone hydrobromide (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a K_i value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrobromide exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies [1] [2] [3] [4] [5].

Cortistatin 29, a neuropeptide, alleviates neuropathic pain and exhibits anti-fibrotic effects. It binds with high affinity to all somatostatin (SS) receptor subtypes, displaying IC 50 values of 2.8 nM for SSTR1, 7.1 nM for SSTR2, 0.2 nM for SSTR3, 3.0 nM for SSTR4, and 13.7 nM for SSTR5, respectively [1] [2] [3] [4].

Angiotensin 1-7 (Ang-(1-7)) acetate, an endogenous heptapeptide from the renin-angiotensin system (RAS), exhibits cardioprotective effects through anti-inflammatory and anti-fibrotic activities in cardiac cells. It inhibits purified canine ACE activity (IC50 = 0.65 μM) and modulates kinin-induced vasodilation by hindering ACE and facilitating nitric oxide release. This compound also prevents Ang II-induced proliferation and hypertrophy in smooth muscle cells and demonstrates antiangiogenic and growth-inhibitory effects on the endothelium [1] [2] [3].

KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.

J-1063 is a selective, orally active and potent inhibitor of ALK5 (IC50: 0.039 μM). J-1063 inhibits inflammatory infiltration, collagen deposition, hepatocyte necrosis and exhibits anti-fibrotic effects. j-1063 has potential for liver fibrosis studies.

FXR agonist 3 is an anti-NASH compound with antifibrotic and anti-fibrotic activity, inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, with an IC50 value of 8.19 μmol L for COL1A1. FXR agonist 3 ameliorates CDAHFD and BDL-induced liver injury in vivo by activating FXR.

(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin, a flavonoid with anti-tyrosinase and anti-fibrotic activity, commonly found in onion, silymarin, French maritime pine bark, and Douglas fir bark. It inhibits collagenase with an IC50 value of 193.3 μM and acts as a free radical scavenger with antioxidant capacity.

Belumosudil mesylate (KD025 mesylate) is a selective ROCK2 inhibitor with IC50 values of 105 nM for ROCK2 and 24 μM for ROCK1, demonstrating anti-fibrotic properties.

Apamin TFA, also known as Apamine TFA, is an 18-amino acid peptide neurotoxin derived from apitoxin (bee venom). It functions as a specifically selective blocker of Ca2+-activated K+ (SK) channels and demonstrates anti-inflammatory and anti-fibrotic activity [1].

SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.

MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor that specifically targets the Mixed Lineage Kinase domain-like (MLKL) protein. It effectively prevents MLKL phosphorylation and oligomerization, which are critical steps in cell necrosis. Additionally, MLKL-IN-6 restrains immune cell death, diminishes adhesion factor expression, exhibits low cytotoxicity, impedes hepatic stellate cell activation, decreases liver fibrosis marker levels, and exerts anti-fibrotic effects [1].

ML-290 is an effective relaxin insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.