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BIO 5192 Sale

目录号 : GC14208

BIO 5192 是一种选择性有效的整合素 α4β1 (VLA-4) 抑制剂 (Kd\u003c10 pM)。

BIO 5192 Chemical Structure

Cas No.:327613-57-0

规格 价格 库存 购买数量
10mg
¥3,150.00
现货
50mg
¥10,080.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

BIO5192 is a small molecule inhibitor of integrin α4β1 with an IC50 value of 1.8 ± 0.7 nM [1].

Integrin α4β1 is important in inflammatory processes. In the inflammatory processes, α4β1 regulates the migration of lymphocytes into inflamed tissues [1].

In assays using cells expressing α4β7, α9β1, α2β1, and αIIbβ3, BIO5192 showed high selectivity for α4β1. The affinity of BIO5192 for α4β1 was 250- to 1000-fold higher than for α4β7 that shared many ligands the same as α4β1. BIO5192 bound even less tightly to α2β1 and αIIbβ3. A significant but low level (KD=140 nM) of binding was seen on α9β1 in buffer containing 1 mM Mn2+ [1].

After 24 h of BIO5192 treatment, the lymphocyte count rose about 1.5-fold. Half as many cells as when TA-2 was given were released into the circulation following the treatment with BIO5192. Data showed that BIO5192 remained bound to 100% of the α4β1 receptors for 24 h and 50% for 48 h. Rats treated with BIO5192 at 30 mg/kg, s.c. showed a 1- to 2-day shift when dosed q.d. and a 3-day delay in the onset of disease EAE when dosed b.i.d. compared with the control groups. The delay in the onset of EAE in the BIO5192-treated group was consistent with the finding that bound BIO5192 would occupy α4β1 long beyond the point at which the BIO5192 was no longer detected in blood [1].

Reference:
[1].  Leone DR, Giza K, Gill A, et al. An assessment of the mechanistic differences between two integrin α4β1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 305(3): 1150-1162.

Chemical Properties

Cas No. 327613-57-0 SDF
化学名 (S)-2-((S)-1-((3,5-dichlorophenyl)sulfonyl)pyrrolidine-2-carboxamido)-4-((S)-4-methyl-2-(N-methyl-2-(4-(3-(o-tolyl)ureido)phenyl)acetamido)pentanamido)butanoic acid
Canonical SMILES ClC1=CC(Cl)=CC(S(=O)(N2[C@H](C(N[C@H](C(O)=O)CCNC([C@H](CC(C)C)N(C)C(CC(C=C3)=CC=C3NC(NC4=CC=CC=C4C)=O)=O)=O)=O)CCC2)=O)=C1
分子式 C38H46Cl2N6O8S 分子量 817.78
溶解度 <81.78mg/ml in DMSO; <40.89mg/ml in 1eq. NaOH 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.2228 mL 6.1141 mL 12.2282 mL
5 mM 0.2446 mL 1.2228 mL 2.4456 mL
10 mM 0.1223 mL 0.6114 mL 1.2228 mL
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