collagen-1

SRI-011381 hydrochloride 是口服具有活力的TGF-β信号通路的激活剂，具有神经保护活性。

SRI011381 是口服具有活力的 TGF-β信号通路的激活剂，具有神经保护活性。

Halofuginone (RU-19110) 是Febrifugine 的衍生物，是一种竞争性脯氨酰-tRNA 合成酶抑制剂。它也是肺血管扩张剂，可激活Kv 通道并阻断电压门控、受体操作和存储操作的钙离子通道。它具有抗炎、抗癌、抗疟疾和抗纤维化作用。

Sinefungin (Adenosyl-Ornithine) 是病毒粒子mRNA (鸟嘌呤-7-)-甲基转移酶、 mRNA (核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。它还抑制SET7/9，通过抑制H3K4甲基化来改善肾纤维化。

Collagen proline hydroxylase inhibitor-1 具有抗纤维增生活性。

Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂，是具有抗炎活性，可减少纤维化，下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。

3-Aminopropionitrile fumarate (2:1) (β-Aminopropionitrile fumarate) 是一种能抑制胶原蛋白(collagen)交联的山黧豆素。

Collagenase Type I 是一种蛋白水解酶，主要靶点是胶原蛋白，能够分解胶原蛋白中的肽键。Collagenase 作为一种潜在的治疗选择来分解突出的椎间盘物质，从而减少对附近神经的压迫。Collagenase 可能有助于过度疤痕组织的分解和重组，潜在地改善组织功能和外观。Collagenase 具有治疗椎间盘突出、瘢痕疙瘩、脂肪团、脂肪瘤以及佩罗尼氏病和手掌纤维瘤病等方面的潜力。

4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。

JTE-952 is a oral, potent active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse

ALK5-IN-82 是一种激活素受体样激酶 5 (ALK5) 的高选择性抑制剂，其IC50值仅为 9.1 nM。该化合物能够有效抑制转化生长因子-β 在人脐静脉内皮细胞中诱导的 α-平滑肌肌动蛋白 (α-SMA)、胶原蛋白 I 以及金属蛋白酶抑制剂 1 (TIMP-1) 和基质金属蛋白酶 13 (MMP‐13) 的表达。因此，ALK5-IN-82 有潜力应用于心脏纤维化的相关研究。

Fibrostat (Compound 5n) 是一种HDAC6选择性抑制剂，通过抑制HDAC6的活性达到其抗纤维化的效果，对HDAC6的IC50为63 nM，并对HDAC1、HDAC3、HDAC5、HDAC8、HDAC10和HDAC11表现出较高选择性。它可以大幅降低成纤维细胞中纤维连接蛋白和胶原1等纤维化标志物的表达。在大鼠灌注心脏及斑马鱼幼体实验中证实其无毒性，Fibrostat 可用于与纤维化相关疾病的研究。

ERBB agonist-1 (Compound EF-1) 是ERBB4的激动剂，能够通过促使 ERBB4 受体二聚化来激活 ERBB4 信号通路，其EC50为10.5 μM。ERBB agonist-1 可促进Akt和ERK1/2的磷酸化，减少心脏成纤维细胞中的胶原蛋白表达，抑制H2O2诱导的心肌细胞死亡以及Ang II诱导的心肌细胞肥大，同时可预防心肌纤维化，在小鼠模型中展现出保护心脏的作用。

FGFRs-IN-1 (Compound A16) 是一种有效的口服FGFR抑制剂，可分别抑制FGFR1、FGFR2、FGFR3和FGFR4，其IC50值为2.3、7、11和163 nM。此外，FGFRs-IN-1 同时抑制VEGFR1/2/3、Abl和Flt3，IC50值分别为61、176、112、26和353 nM，然而对CYP酶的抑制作用较弱。该化合物可降低α-SMA和胶原蛋白I (collagen I) 的表达，并在TGF-β1刺激的A549细胞中抑制上皮-间质转化 (EMT)。在Bleomycin诱导的小鼠肺纤维化模型及CCl4诱导的小鼠肝纤维化模型中，FGFRs-IN-1 显示出抗炎活性。

ATX-IN-1 (compound 35) 是一种 ATX 抑制剂 (IC50=0.7 nM)，展现出抗炎活性。该化合物能够通过抑制 TGF-β/Smad 通路和减少胶原蛋白沉积来缓解 Bleomycin 引发的小鼠纤维化模型。ATX-IN-1 在口服时具备良好的生物利用率 (F=69.5%) 和微粒稳定性。

Galectin-3-IN-6 (Compound 12) 是一种口服活性的半乳糖凝集素-3 (Gal-3) 抑制剂，对 Gal-3 的 IC50 为 12 nM，Kd 为 13 nM。在 CCl4 诱导的小鼠急性肝损伤和纤维化模型中，该化合物能够显著降低纤维化标志物胶原蛋白-1 和 α-平滑肌肌动蛋白 (αSMA) 的水平，分别降低 64% 和 71%，显示出良好的抗纤维化活性。Galectin-3-IN-6 适用于纤维化疾病、癌症以及心血管疾病的研究。

1-Methylnicotinamide是nicotinamide的活性代谢产物，由nicotinamide N-methyltransferase催化形成。1-Methylnicotinamide以浓度依赖的方式诱导人脐静脉内皮细胞（HUVECs）分泌一氧化氮。当以30 mg/kg剂量给药时，能增加大鼠血浆6-keto-prostaglandin F1α水平，并在相同剂量下抑制大鼠胶原诱导的血栓形成。

SP-100030 是一种有效的 NF-κB 和激活蛋白-1 (AP-1) 双抑制剂 (IC50 分别为 50 和 50 nM)。SP-10003 抑制 Jurkat 和其他T 细胞系产生的 IL-2、IL-8 和 TNF-α 的产生。SP-100030 降低小鼠胶原性关节炎 (CIA)。

Allylpyrocatechol is an antioxidant. Allylpyrocatechol attenuates collagen-induced arthritis via attenuation of oxidative stress secondary to modulation of the MAPK, JAK/STAT, and Nrf2/HO-1 pathways.

Diethyl pyimDC is an inhibitor of human collagen prolyl 4-hydroxylase 1 (CP4H1).

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019). SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).

Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximately 90% when used at a concentration of 10 μg/ml. It also inhibits fMLF-induced neutrophil aggregation and degranulation by 55 and 68%, respectively, when used at a concentration of 5 μM, similar to arachidonic acid .3 Oleic acid (60 μM) induces release of intracellular calcium in human platelets.4

4-hydroxy Valsartan is a major metabolite of the angiotensin II type 1 (AT1) receptor antagonist valsartan . It reduces platelet aggregation induced by epinephrine and collagen but not ADP in human whole blood.