| Cas No.: | 852948-13-1 |
| Chemical Name: | MB-07811 (VK-2809) |
| Synonyms: | MB-07811;VK-2809;MB07811;VK2809;MB 07811;VK 2809 |
| SMILES: | OC1=CC=C(CC2=C(C)C=C(OC[P@]3(OCC[C@@H](C4=CC=CC(Cl)=C4)O3)=O)C=C2C)C=C1C(C)C |
| Formula: | C28H32ClO5P |
| M.Wt: | 514.977 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Publication: | [1]. Cable EE, et al. Reduction of hepatic steatosis in rats and mice after treatment with aliver-targeted thyroidhormone receptor agonist. Hepatology. 2009 Feb;49(2):407-17. [2]. Erion MD, et al. Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5. |
| Description: | MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist[1]. MB-07811 has cholesterol and triglycerides lowering activity[2]. |
| Target: | Thyroid hormone receptor-β[2] |
| In Vivo: | MB-07811 (0.3-30 mg/kg; orally once daily for 14 days) reduces cholesterol and triglycerides in diet-induced obese mice[2]. Animal Model: 4-week-old male C57BL/6 mice (diet-induced obese (DIO) mice)[2] Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Orally once daily; 14 days Result: Reduced total plasma cholesterol, and reduced plasma triglycerides (40%) at the highest doses. |
| In Vitro: | MB-07811 is potential for liver targeting with a low affinity for thyroid hormone receptors (TRβ Ki = 14.6 ± 0.5 μM; TRα Ki = 12.5 ± 0.6 μM)[2]. |
| References: | [1]. Cable EE, et al. Reduction of hepatic steatosis in rats and mice after treatment with aliver-targeted thyroidhormone receptor agonist. Hepatology. 2009 Feb;49(2):407-17. [2]. Erion MD, et al. Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5. |
MSDS
COA
| LOT NO. | DOWNLOAD |
|
|
|
| 2018-0101 |
|
| 2018-0101 |
|