CXCR7 modulator 2

小分子

CXCR7 调制器 2

CXCR7 modulator 2

C650931-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 ( CXCR7 ), with a K i of 13 nM. In Vitro CXCR7 modulator 2 (compound 18) demonstrates potent CXCR7-binding affinity (K i =13 nM) and β-arrestin activity (EC 50 =11 nM). CXCR7 modulator 2 also exhibits improved selectivity in the GPCR panel and an improved therapeutic index in the hERG patch-clamp assay in comparison with 11c. CXCR7 modulator 2 exhibits moderate to high in vitro turn over in both NADPH-supplemented mouse-liver microsomes (MLM, 93 μL/min/mg) and hepatocytes (28 μL/min per million cells), shows poor passive absorptive permeability in the MDCK II-permeability assay, and has good aqueous solubility. CXCR7 modulator 2 is rapidly absorbed with a mean maximal plasma concentration (C max ) of 682 ng/mL, which occurrs at 0.25 h (T max ). The corresponding mean area under the plasma-concentration-versus-time profile (AUC) is 740 ng/mL/h. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo The administration of isoproterenol for 9 days leads to the development of cardiac fibrosis, as attested by the approximately 4-fold increase in collagen deposition relative to that in the control, which is detected by picrosirius-red staining. Treatment with CXCR7 modulator 2 results in a statistically significant reduction in cardiac fibrosis, thereby demonstrating the protective role of CXCR7 modulation with CXCR7 modulator 2 in an isoproterenol-induced cardiac injury . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:CXCR7 13 nM (Ki)

CXCR7 调节剂 2 是一种 C-X-C 趋化因子受体 7 型（CXCR7）调节剂，其 K i 为 13 nM。

2227426-37-9

C29H42N6O3

522.68 g/mol

134694953

CCC1=C(C2=NC=CN2C=C1)N3CCCN(CC3)[C@@H](CC(=O)N)C4CCN(CC4)C(=O)[C@H]5C[C@@H]6CC[C@H]5O6

(3S)-3-[4-(7-ethylimidazo[1,2-a]pyridin-8-yl)-1,4-diazepan-1-yl]-3-[1-[(1R,2S,4S)-7-oxabicyclo[2.2.1]heptane-2-carbonyl]piperidin-4-yl]propanamide

1S/C29H42N6O3/c1-2-20-6-12-34-15-9-31-28(34)27(20)33-11-3-10-32(16-17-33)24(19-26(30)36)21-7-13-35(14-8-21)29(37)23-18-22-4-5-25(23)38-22/h6,9,12,15,21-25H,2-5,7-8,10-11,13-14,16-19H2,1H3,(H2,30,36)/t22-,23-,24-,25+/m0/s1

CERHKHQEGFSIHF-OJJQZRKESA-N

CCC1=C(C2=NC=CN2C=C1)N3CCCN(CC3)C(CC(=O)N)C4CCN(CC4)C(=O)C5CC6CCC5O6

134694953

DMSO : 250 mg/mL (478.30 mM; Need ultrasonic)