BVT 2733 is a small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1(11β-HSD1).
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产品名称 | Dehydrogenase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Trilostane | ✔ | 99+% | |||||||||||||||||
AGI-6780 |
+++
IDH2 R140Q mutant, IC50: 23 nM |
99%+ | |||||||||||||||||
Gimeracil | ✔ | 98% | |||||||||||||||||
AGI-5198 |
++
R132C-IDH1, IC50: 0.16 μM R132H-IDH1, IC50: 70 nM |
99%+ | |||||||||||||||||
SW033291 |
++++
15-PGDH, IC50: 1.5 nM 15-PGDH, Ki: 0.1 nM |
99%+ | |||||||||||||||||
Mycophenolic acid | ✔ | 99+% | |||||||||||||||||
Fomepizole | ✔ | 98% | |||||||||||||||||
Leflunomide | ✔ | 98% | |||||||||||||||||
3-Nitropropanoic acid | ✔ | 99%+ | |||||||||||||||||
Isovaleramide | ✔ | 99% | |||||||||||||||||
Mycophenolate Mofetil |
+++
Inosine monophosphate dehydrogenase II, IC50: 27 nM Inosine monophosphate dehydrogenase I, IC50: 39 nM |
98% | |||||||||||||||||
MK-8245 |
++++
SCD1 (mouse), IC50: 1 nM SCD1 (rat), IC50: 3 nM |
99%+ | |||||||||||||||||
Vidofludimus |
++
Human DHODH, IC50: 134 nM |
99%+ | |||||||||||||||||
Emodin | ✔ | 98% | |||||||||||||||||
Ivosidenib | ✔ | 98% | |||||||||||||||||
NCT-501 |
++
ALDH1A1, IC50: 40 nM |
98% | |||||||||||||||||
Gossypol | ✔ | 99%+ | |||||||||||||||||
Devimistat | ✔ | 98% | |||||||||||||||||
Disulfiram | ✔ | 98%+ | |||||||||||||||||
Enasidenib |
++++
IDH2, IC50: 12 nM |
98% | |||||||||||||||||
PluriSIn 1 | ✔ | 99%+ | |||||||||||||||||
ML390 |
+
DHODH, IC50: 0.56 μM |
99%+ | |||||||||||||||||
Teriflunomide | ✔ | 99%+ | |||||||||||||||||
Daidzin |
+++
ALDH-Ⅰ, Ki: 20 nM |
98+% | |||||||||||||||||
18β-Glycyrrhetinic acid | ✔ | 99% | |||||||||||||||||
RRx-001 | ✔ | 95% | |||||||||||||||||
NCT-503 |
+
PHGDH, IC50: 2.5 μM |
99%+ | |||||||||||||||||
Vorasidenib | ✔ | 99%+ | |||||||||||||||||
Ammonium Glycyrrhizinate(x:1) | ✔ | 98+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | BVT.2733 is a new, small molecule, non-steroidal, isoform-selective inhibitor of mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). It lowered hepatic PEPCK and glucose-6-phosphatase mRNA, blood glucose and serum insulin concentrations compared with vehicle treated mice[4]. BVT-2733 exhibited an anti-inflammatory effect. BVT.2733 treatment could not only decrease body weight and improve metabolic homeostasis, but also suppress the inflammation of adipose tissue in diet-induced obese mice, shown as the down-regulated the expression of inflammation-related genes MCP-1, TNF-α and the number of infiltrated macrophages in vivo[5]. Oral administration of 100mg/kg BVT-2733 twice daily for 2 weeks attenuated the arthritis severity and anti-CII level in CIA (collagen-induced arthritis) mice, decreased the levels of serum TNF-α, IL-1β, IL-6 and IL-17, and also significantly reduced synovial inflammation and joint destruction[6]. |
Dose | Mice: 100 mg/kg[3] (p.o.), 200 mg/kg[4] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.66mL 2.33mL 1.17mL |
23.31mL 4.66mL 2.33mL |
CAS号 | 376640-41-4 |
分子式 | C17H21ClN4O3S2 |
分子量 | 428.96 |
SMILES Code | O=S(C1=CC=CC(Cl)=C1C)(NC2=NC(CC(N3CCN(C)CC3)=O)=CS2)=O |
MDL No. | MFCD13152134 |
别名 | |
运输 | 蓝冰 |
InChI Key | YDPRNGAPPNPYQQ-UHFFFAOYSA-N |
Pubchem ID | 6918651 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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