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Almotriptan

Name: Almotriptan
Brand: TargetMol
SKU: T21231
Price: 178 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.85%

货号 T21231Cas号 154323-57-6

别名 阿莫曲坦, 阿莫曲普坦, LAS 31416

Almotriptan (LAS 31416) 是一种用于研究偏头痛的5-HT1B/1D 受体激动剂。

Almotriptan

一键复制产品信息

很棒

纯度: 99.85%

货号 T21231 别名 阿莫曲坦, 阿莫曲普坦, LAS 31416Cas号 154323-57-6

Almotriptan (LAS 31416) 是一种用于研究偏头痛的5-HT1B/1D 受体激动剂。

规格	价格	库存
1 mg	¥ 178	现货
5 mg	¥ 349	现货
10 mg	¥ 498	现货
25 mg	¥ 1,050	现货
50 mg	¥ 1,560	现货
100 mg	¥ 2,320	现货
1 mL x 10 mM (in DMSO)	¥ 388	现货

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纯度: 99.85%

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COA HNMR LCMS 产品操作手册

产品介绍

Almotriptan AI Summary

Almotriptan demonstrates a broad spectrum of pharmacological and bioactive properties with significant relevance for both therapeutic applications and pharmacokinetic studies. It exhibits an oral bioavailability of 70% in humans, indicating efficient absorption when administered orally. Pharmacokinetic parameters include a volume of distribution (Vdss) of 2.2 L/kg, a half-life (T1/2) of 3.4 hours, and total body clearance (CL) of 8.9 mL/min/kg, with renal clearance (CLr) at 5.79 mL/min/kg, denoting notable elimination via the kidneys. Additionally, it has a fraction unbound (Fu) of 0.6 after intravenous administration. The compound shows a human intestinal absorption rate with a log10(%HIA +10) value of 1.929, underscoring its absorption potential. Bioactively, Almotriptan is potent against Plasmodium falciparum strains with inhibition ranges from 2.1 nM to 3346.9 nM. It also modulates Lamin A splicing, acts as a GLP-1 receptor agonist, and inhibits Ebola virus entry, with AC50 values ranging from 1.995 μM to 39810.7 nM. While showing negligible antiviral activity against SARS-CoV-2 in HRCE cells, an IC50 value greater than 20000.0 nM was observed inhibiting cytotoxicity in VERO-6 cells. Liver toxicity assessments reveal a severity class index for drug-induced liver injury of 0.0, indicating no liver toxicity. Almotriptan inhibits sodium fluorescein uptake in OATP1B3 and OATP1B1-transfected CHO cells by 94.33% and 95.85% respectively. Furthermore, it shows limited inhibitory activity on human HDAC6 enzyme (5.9% with commercial substrates, 2.3% with custom substrates). Its binding affinity spans multiple receptors and enzymes, including HRH1, KCNH2, SLC6A3, CHRNA4, and OPRK1, with agonist and antagonist activities across various receptors such as HTR1A, HTR2A, ADRB2, PPARG, CHRM2, and GABRA1. Inhibition extends to targets ABCB11, MAOA, PTGS2, and PDE4D, reflecting a complex bioactivity profile across various molecular targets..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述

Almotriptan (LAS 31416) is a 5-HT1B/1D-receptor agonist used to treat migraine.Almotriptan is a triptan drug for treatment of migraine headaches.Binding of the drug to the receptor leads to vasoconstriction of the cranial blood vessels and thus affects the redistribution of cranial blood flow. Almotriptan significantly increases cerebral blood flow and reduces blood flow through extracerebral cranial vessels.

别名

阿莫曲坦, 阿莫曲普坦, LAS 31416

化学信息

分子量	335.46
分子式	C₁₇H₂₅N₃O₂S
CAS No.	154323-57-6
Smiles	CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N3CCCC3)cc12
密度	1.27 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 65 mg/mL (193.76 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.96 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9810 mL	14.9049 mL	29.8098 mL	149.0491 mL
5 mM	0.5962 mL	2.9810 mL	5.9620 mL	29.8098 mL
10 mM	0.2981 mL	1.4905 mL	2.9810 mL	14.9049 mL
20 mM	0.1490 mL	0.7452 mL	1.4905 mL	7.4525 mL
50 mM	0.0596 mL	0.2981 mL	0.5962 mL	2.9810 mL
100 mM	0.0298 mL	0.1490 mL	0.2981 mL	1.4905 mL