BMS813160
BMS813160 Basic information
- Product Name:
- BMS813160
- Synonyms:
-
- CS-2742
- BMS-813160;BMS813160;BMS 813160
- N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide
- BMS813160
- Acetamide, N-[(1R,2S,5R)-5-[(1,1-dimethylethyl)amino]-2-[(3S)-3-[[7-(1,1-dimethylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl]amino]-2-oxo-1-pyrrolidinyl]cyclohexyl]-
- Inhibitor,CC chemokine receptor,CCR,dual antagonist,peritonitis,CD11b,BMS-813160,inflammation,CTX,thioglycollate,BMS813160,inhibit,mouse,oral
- BMS-813160, 10 mM in DMSO
- BMS-585059
- CAS:
- 1286279-29-5
- MF:
- C25H40N8O2
- MW:
- 484.64
- Mol File:
- 1286279-29-5.mol
BMS813160 Chemical Properties
- Density
- 1.31±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO:61.0(Max Conc. mg/mL);125.86(Max Conc. mM)
Ethanol:97.0(Max Conc. mg/mL);200.14(Max Conc. mM) - form
- A crystalline solid
- pka
- 15.46±0.60(Predicted)
- color
- White to off-white
- InChIKey
- CMVHFGNTABZQJU-HCXYKTFWSA-N
- SMILES
- C(N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC2N3N=C(C(C)(C)C)C=C3N=CN=2)C1=O)(=O)C
BMS813160 Usage And Synthesis
Description
BMS 813160 is a dual antagonist of chemokine receptor 2 (CCR2) and CCR5 (IC50s = 6.2 and 3.6 nM, respectively, in radioligand binding assays). It inhibits chemotaxis induced by the CCR2 ligand MCP-1 in THP-1 cells the CCR5 ligand MIP-1β in isolated peripheral T cells with IC50 values of 0.8 and 1.1 nM, respectively. BMS 813160 inhibits peritoneal monocyte and macrophage infiltration in an hCCR-2 KI mouse model of thioglycolate-induced peritonitis, with 54% inhibition when administered at a dose of 50 mg/kg twice per day.
Uses
BMS-813160, a dual CCR2/CCR5 chemokine antagonist.
in vivo
BMS-813160 (10-160 mg/kg; p.o. twice a day for two days) inhibits the migration of inflammatory monocytes and macrophages in mouse thioglycollate-induced peritonitis model, and shows excellent oral bioavailability[2].
| Animal Model: | Human-CCR2 knock-in C57BL/6 male mice with thioglycollate injection[2] |
| Dosage: | 10, 50 and 160 mg/kg |
| Administration: | Oral gavage; 10-160 mg/kg twice a day; for two days |
| Result: | Dose-dependently reduced inflammatory monocyte and macrophage infiltration in the peritoneum. |
IC 50
CCR5: 3.6 nM (IC50); CCR2: 6.2 nM (IC50)
References
[1] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[2] NORMAN P. A dual CCR2/CCR5 chemokine antagonist, BMS-813160? Evaluation of WO2011046916.[J]. Expert Opinion on Therapeutic Patents, 2011, 21 12: 1919-1924. DOI: 10.1517/13543776.2011.622750
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