Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
BMS-1001 is a novel and potent PD-1/PD-L1 interaction inhibitor. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.
ln Vitro |
LPA1+ cells and lung sections showed concentration-dependent shifts of [18F]BMT-083133-bound BMS-986020 sodium (0.1-10 nM; preincubation). The percentage displacement of the lungs of healthy mice, bleomycin mice, and IPF mice was 18%, 24%, and 31%, at a dose of 0.1 nM, respectively. The displacement percentages were 73%, 76%, and 64% at 10 nM, in that order. Developed as a translational research tool to assess the pulmonary LPA1 engagement of BMS-986020 using in vitro autoradiography (ARG), [18F]BMT-083133 is a radioligand targeting LPA1 [4].
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References |
[1]. Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7.
[2]. Glenn Rosen, et al. LPA1 antagonists BMS-986020 and BMS-986234 for idiopathic pulmonary fibrosis: Preclinical evaluation of hepatobiliary homeostasis. European Respiratory Journal. [3]. Palmer SM, et al. Randomized, Double-Blind, Placebo-Controlled, Phase 2 Trial of BMS-986020, a Lysophosphatidic Acid Receptor Antagonist for the Treatment of Idiopathic Pulmonary Fibrosis. Chest. 2018 Nov;154(5):1061-1069. [4]. Adrienne Pena, et al. Autoradiographic evaluation of [18F]BMT-083133, a lysophosphatidic acid receptor 1 (LPA1) radioligand. The jornal of nuclear medicine. |
Molecular Formula |
C29H25N2NAO5
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Molecular Weight |
504.50897860527
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CAS # |
1380650-53-2
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SMILES |
[Na+].[O-]C(C1(C2C=CC(C3C=CC(C4=C(C(C)=NO4)NC(=O)O[C@H](C)C4C=CC=CC=4)=CC=3)=CC=2)CC1)=O
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InChi Key |
UWNXGZKSIKQKAH-SSEXGKCCSA-N
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InChi Code |
InChI=1S/C35H34N2O7/c1-22-13-28(18-37-30(19-38)35(39)40)33(43-20-25-6-3-5-24(14-25)17-36)16-32(22)44-21-27-7-4-8-29(23(27)2)26-9-10-31-34(15-26)42-12-11-41-31/h3-10,13-16,30,37-38H,11-12,18-21H2,1-2H3,(H,39,40)/t30-/m1/s1
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Chemical Name |
(2-((3-Cyanobenzyl)oxy)-4-((3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-methylbenzyl)oxy)-5-methylbenzyl)-D-serine
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Synonyms |
BMS-1001 BMS1001 BMS1001 BMS-1001 free base
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~150 mg/mL (~297.32 mM)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9821 mL | 9.9106 mL | 19.8212 mL | |
5 mM | 0.3964 mL | 1.9821 mL | 3.9642 mL | |
10 mM | 0.1982 mL | 0.9911 mL | 1.9821 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.