貨號	規格	價格	上海	北京	武漢	南京
S89693-5mg	98.0%	￥900.00 S89693-5mg ￥900.00 現貨	6 6	-	-	-
S89693-10mg	98.0%	￥1600.00 S89693-10mg ￥1600.00 現貨	7 7	-	-	-
S89693-25mg	98.0%	￥3500.00 S89693-25mg ￥3500.00 現貨	6 6	-	-	-
S89693-100mg	≥98%	￥13100.00 S89693-100mg ￥13100.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM

產品描述：

靶點：

IC50: 395 nM (human calpain 1);CysteineProtease

體外研究：

(1S,2R)-Alicapistat exihibits inadequate CNS-penetration concentrations to obtain a pharmacodynamic effect.
Calpain 1 (μ-calpain) and 2 (m-calpain) expression in a calcium-dependent manner with μ-molar or m-molar calcium concentrations required for their respective activation, respectively. (1S,2R)-Alicapistat (compound 22) (100 nM) prevents Aβ oligomer-induced deficits in synaptic transmission in rat.
(1S,2R)-Alicapistat (compound 22) (385 nM) diplays efficacy with respect to prevention of NMDA-induced neurodegeneration and A-induced synaptic dysfunction.
(1S,2R)-Alicapistat (9-21 nM) has the CSF concentrations without reaching the IC50 for calpain inhibition and shows no dose-limiting toxicities (DLTs) in the broad populations studies.

體內研究：

(1S,2R)-Alicapistat (compound 22) (iv or po; 1-3 mg/kg) shows moderate mean plasma clearance values (CLp) in mouse, rat, and dog (0.13-1.04 L/hr.kg), while high in monkey (1.98 L/hr.kg). Mean steady-state volume of distribution values (Vss) were moderate in mouse, dog, and monkey (0.64-1.8 L/kg), but higher in rat (3.4 L/kg). The plasma elimination half-life (t1/2) was shortest in dog (1.7 hours), followed by 2.3 hours in monkey and approximately 6.0 hours in mouse and rat. Oral bioavailability (F) values were high in mouse, rat, and dog (>80%), while moderate in monkey (14%).

參考文獻：

1. Lon HK, et al. Pharmacokinetics, Safety, Tolerability, and Pharmacodynamics of Alicapistat, a Selective Inhibitor of Human Calpains 1 and 2 for the Treatment of Alzheimer Disease: An Overview of Phase 1 Studies. Clin Pharmacol Drug Dev. 2019 Apr. 8(3):290

2. Jantos K, et al. Discovery of ABT-957: 1-Benzyl-5-oxopyrrolidine-2-carboxamides as selective calpain inhibitors with enhanced metabolic stability. Bioorg Med Chem Lett. 2019 Aug 1. 29(15):1968-1973.

3. Jastaniah A, Gaisina IN, Knopp RC, Thatcher GRJ. Synthesis of α-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents. ChemMedChem. 2020 Dec 3. 15(23):2280-2285.

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.307 ml	11.534 ml	23.068 ml
5 mM	0.461 ml	2.307 ml	4.614 ml
10 mM	0.231 ml	1.153 ml	2.307 ml
50 mM	0.046 ml	0.231 ml	0.461 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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