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Vonoprazan (TAK-438 free base) 是有一种口服活性的 钾竞争性酸阻断剂，抑制 H+, K+-ATPase的 IC50 值为 19 nM。
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Vonoprazan Chemical Structure
CAS No. : 881681-00-1
| Description |
Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM. |
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| Molecular Weight |
345.39 |
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| Formula |
C₁₇H₁₆FN₃O₂S |
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| CAS No. |
881681-00-1 |
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| SMILES |
O=S(N1C=C(CNC)C=C1C2=CC=CC=C2F)(C3=CC=CN=C3)=O |
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| Shipping |
Room temperature in continental US; may vary elsewhere. |
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| Storage |
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| Solvent & Solubility |
In Vitro:
DMSO : ≥ 33 mg/mL (95.54 mM) * "≥" means soluble, but saturation unknown.
Preparing
Stock Solutions
*
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。 |
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| References |
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MedChemExpX品牌 历史介绍:苏州蚂蚁淘生物科技有限公司，作为一家生命科学领域的高科技生物公司，目前代理销售二十多家欧美著名生物技术公司的产品，覆盖了免疫学、细胞生物学、分子生物学、药物筛选、生物制药、食品检测、疫苗生产等领域。
Avexitide (Synonyms: Exendin (9-39)) 目录号: HY-P0264 纯度: 99.70%Data Sheet SDS 产品使用指南 Avexitide (Exendin (9-39)) 是特异竞争性的 glucagon-like peptide-1 (GLP-1) 受体拮抗剂。 MCE 的所有产品仅用作科学研究，我们不为任何个人用途提供产品和服务 Avexitide Chemical Structure CAS No. : 133514-43-9 Size Price Stock Quantity 500 μg ￥1700 In-stock 0 1 2 3 4 5 6 7 1 mg ￥2700 In-stock 0 1 2 3 4 5 6 7 5 mg ￥8100 In-stock 0 1 2 3 4 5 6 7 10 mg Get quote 50 mg Get quote or大包装询价 Customer Review MCE 顾客使用本产品发表的科研文献 •Br J Pharmacol. 2020 Mar 30. •Exp Biol Med (Maywood). 2019 Sep 11:1535370219876531. Avexitide 相关产品 •Related Screening Libraries: Clinical Compound Library Plus Drug Repurposing Compound Library Plus Bioactive Compound Library Plus •Related Small Molecules: Exendin-4 Liraglutide Glucagon Adomeglivant Semaglutide TFA GLP-1(7-36) Acetate MK 0893 GLP-1(7-37) Tirzepatide hydrochloride Lixisenatide BETP GLP-1 receptor agonist 1 GRA Ex-25 LGD-6972 Taspoglutide GLP-1 receptor agonist 2 GLP-2(1-33)(human) Glucagon-like peptide 1 (1-37), human TFA GLP-1 moiety from Dulaglutide NNC-0640 PF-06291874 Cotadutide acetate Glucagon receptor antagonists-3 Human growth hormone-releasing factor Exendin-3/4 (59-86) FTSDVSKQMEEEAVRLFIEWLKNGGPSSGAPPPS Glucagon receptor antagonists-1 生物活性 实验参考方法 纯度 & 产品资料 参考文献 Description Avexitide (Exendin (9-39)) is a specific and competitive GLP-1 receptor antagonist. In Vitro GLP-1 plays a role in the control of fasting glucose. Avexitide (Exendin (9-39)), a truncated form of the GLP-1 agonist exendin-4, is a specific GLP-1 receptor antagonist[1]. In Vivo Continuous subcutaneous infusion of Avexitide (Exendin (9-39)) significantly raises fasting blood glucose levels in SUR-1 -/- mice without affecting glucose tolerance[2]. Clinical Trial NCT Number Sponsor Condition Start Date Phase NCT03246451 University Hospital, Gentofte, Copenhagen|University of Copenhagen Glucose Metabolism Disorders July 1, 2017 Not Applicable NCT01729299 David Dalessio|National Institutes of Health (NIH)|University of Cincinnati Diabetes April 2013 Not Applicable NCT02996812 Tracey McLaughlin|Stanford University Hyperinsulinemia Hypoglycemia April 2015 Phase 1 Molecular Weight 3369.76 Formula C₁₄₉H₂₃₄N₄₀O₄₇S CAS No. 133514-43-9 Sequence Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 Sequence Shortening DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 SMILES [DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2] Shipping Room temperature in continental US; may vary elsewhere. Storage Powder -80°C 2 years -20°C 1 year In solvent -80°C 6 months -20°C 1 month Solvent & Solubility In Vitro: H2O : 50 mg/mL (14.84 mM; Need ultrasonic) Preparing Stock Solutions ConcentrationSolventMass 1 mg 5 mg 10 mg 1 mM 0.2968 mL 1.4838 mL 2.9676 mL 5 mM 0.0594 mL 0.2968 mL 0.5935 mL 10 mM 0.0297 mL 0.1484 mL 0.2968 mL * 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, 6 months; -20°C, 1 month。 -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。 References [1]. Calabria AC, et al. GLP-1 receptor antagonist exendin-(9-39) elevates fasting blood glucose levels in congenital owing to inactivating mutations in the ATP-sensitive K+ channel. Diabetes. 2012 Oct;61(10):2585-91. [2]. De León DD, et al. Exendin-(9-39) corrects fasting hypoglycemia in SUR-1-/- mice by lowering cAMP in pancreatic beta-cells and inhibiting secretion. J Biol Chem. 2008 Sep 19;283(38):25786-93.
