| 價(jià)格 | ¥24800 | ¥30500 | ¥20000 |
| 包裝 | 50mg | 100mg | 25mg |
| 最小起訂量 | 25mg |
| 發(fā)貨地 | 上海 |
| 更新日期 | 2026-06-29 |
| 中文名稱:化合物 MK-4256 | 英文名稱:MK-4256 |
| CAS:1104599-69-0 | 品牌: TargetMol |
| 產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 產(chǎn)品類別: 抑制劑 | |
| 貨號(hào): T001|T16095 |
| 名稱 | MK-4256 |
| 描述 | MK-4256 is an effective and selective SSTR3 antagonist (IC50s: 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively). |
| 體外活性 | MK-4256 is tested in functional antagonist assays against SSTR4 and SSTR5. The IC50 values are greater than 5 μM (at least 5000-fold selectivity)[1]. MK-4256 inhibits radiolabeled MK-499 binding of the hERG channel (IC50=1.74 μM). MK-4256 has excellent selectivity against other SSTR subtypes based on in vitro assays and it also has IC50s >2 μM for SSTR1 and SSTR2, in human receptor binding assays. Although the binding IC50 values on SSTR4 and SSTR5 are below 1 μM, there is still >500-fold selectivity. MK-4256 exhibits 50% blockade of hERG at 3.4 μM concentration, in a functional patch-clamp assay[2]. |
| 體內(nèi)活性 | MK-4256 decreases the glucose excursion from 0.003 to 10 mg/kg in a dose-dependent manner. MK-4256 decreases glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses of MK-4256 (0.03 mg/kg; p.o.) demonstrates exceptional SSTR3-mediated glucose-lowering efficacy in the mouse oGTT model with minimal hypoglycemia risk. MK-4256 (1 mg/kg; p.o.) achieves complete ablation of glucose excursion (109%). The plasma Cmax of MK-4256 is determined from parallel mouse PK studies. MK-4256 achieves Cmax of 7, 88, and 493 nM, respectively, at 0.01, 0.1, and 1 mg/kg oral dose [1]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 100 mg/mL (202.22 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 4 mg/mL (8.09 mM), Sonication is recommended. |
| 關(guān)鍵字 | mouse SSTR3 | MK-4256 | MK4256 | MK 4256 | human SSTR3 |
| 相關(guān)產(chǎn)品 | [Tyr3]Octreotate | BIM-23190 aceate | Lanreotide acetate | CYN 154806 TFA | 2-Aminoethanethiol | Somatostatin acetate | L-797,591 hydrochloride | L-796,778 | Octreotide | Octreotide Acetate | Cortistatin-14 acetate | AGI-43192 |
| 成立日期 | 2013-04-18 (14年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
| 員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
| 主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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|---|---|---|---|---|
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2026-07-29 | |
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VIP6年
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