L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-
![L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Structure](CAS/20210305/GIF/2411440-41-8.gif)
- CAS No.
- 2411440-41-8
- Chemical Name:
- L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-
- Synonyms
- JR14a;L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]-;inflammation,Inhibitor,inhibit,C3a,JR-14a,Complement System,JR14a,complement;5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-l-arginine hydrochloride;(S)-2-(5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carboxamido)-5-guanidinopentanoic acid
- CBNumber:
- CB69270798
- Molecular Formula:
- C25H26Cl2N4O3S
- Molecular Weight:
- 533.47
- MDL Number:
- MFCD34471093
- MOL File:
- 2411440-41-8.mol
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Chemical Properties,Uses,Production
Biological Activity
JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation[1]. JR14a (0.1 nM-100 μM) inhibits C3a-induced intracellular Ca2+ release in human monocyte-derived macrophages, with an IC50 of 10 nM[1].JR14a (0.1 nM-100 μM) is metabolically stable to exposure over 1 h to rat liver microsomes[1].JR14a (0.1 nM-100 μM) inhibits C3a-induced β-hexosaminidase secretion in human LAD2 mast cells, with an IC50 of 8 nM[1]. JR14a (10 mg/kg; p.o. 2 h prior) reduces paw swelling by 65% over control at 30 min after agonist injection in acute rat paw model of inflammation and edema[1].JR14a (1 mg/kg; i.v.) exhibits elimination half-life (191 min), clearance (4.4 mL/min/kg) and AUC (3795 ng?h/mL) in rats[1].JR14a (10 mg/kg; p.o.) exhibits Cmax (88 ng/mL), Tmax (300 min) and AUC (478 ng?h/mL) in rats[1].
References
[1]. Rowley JA, et, al. Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity. J Med Chem. 2020 Jan 23;63(2):529-541.
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
L-Arginine, N2-[[5-[bis(4-chlorophenyl)methyl]-3-methyl-2-thienyl]carbonyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 4692 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3453 | 58 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9708 | 58 |
| Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9874 | 58 |
| Beijing Solarbio Science & Tecnology Co., Ltd. | 010-50973130 4009686088 | 3193328036@qq.com | China | 29795 | 68 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9412 | 58 |