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(S)-KT109 Sale

目录号 : GC41738

An isomer of KT109

(S)-KT109 Chemical Structure

Cas No.:2055172-61-5

规格 价格 库存 购买数量
500μg
¥1,284.00
现货
1mg
¥2,449.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

(S)-KT109 is the (S) isomer of the diacylglycerol lipase β (DAGLβ) inhibitor KT109 . (S)-KT109 is a less potent inhibitor of DAGLβ (IC50 = 39.81 nM), DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol (IC50 = 794.3 nM), and α/β-hydrolase domain-containing protein 6 (ABHD6; IC50 = 630.9 nM) than (R)-KT109 .

Chemical Properties

Cas No. 2055172-61-5 SDF
Canonical SMILES O=C(N1N=NC(C2=CC=C(C3=CC=CC=C3)C=C2)=C1)N4[C@H](CC5=CC=CC=C5)CCCC4
分子式 C27H26N4O 分子量 422.5
溶解度 DMF: 10 mg/mL,DMSO: 10 mg/mL 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3669 mL 11.8343 mL 23.6686 mL
5 mM 0.4734 mL 2.3669 mL 4.7337 mL
10 mM 0.2367 mL 1.1834 mL 2.3669 mL
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Research Update

Monoacylglycerol Lipase Inhibition Using JZL184 Attenuates Paw Inflammation and Functional Deficits in a Mouse Model of Inflammatory Arthritis

Cannabis Cannabinoid Res 2021 Jun;6(3):233-241.PMID:34042520DOI:PMC8217598

Background: Patients with rheumatoid arthritis (RA) experience joint swelling and cartilage destruction resulting in chronic pain, functional disability, and compromised joint function. Current RA treatments, including glucocorticoid receptor agonists, produce adverse side effects and lack prolonged treatment efficacy. Cannabinoids (i.e., cannabis-like signaling molecules) exert anti-inflammatory and analgesic effects with limited side effects compared to traditional immunosuppressants, making them excellent targets for the development of new arthritic therapeutics. Monoacylglycerol lipase (MAGL) inhibition reduces inflammation in mouse models of acute inflammation, through cannabinoid receptor dependent and independent pathways. The current study investigated the efficacy of inhibiting synthetic and catabolic enzymes that regulate the endocannabinoid 2-arachidonoylglycerol (2-AG) in blocking paw inflammation, pain-related behaviors, and functional loss caused by collagen-induced arthritis (CIA). Methods: Male DB1A mice subjected to CIA were administered the glucocorticoid agonist dexamethasone (DEX), MAGL inhibitor JZL184 (8 or 40 mg/kg, S.c.), alone or in combination, or diacylglycerol lipase β (DAGLβ) inhibitor KT109 (40 mg/kg, S.c.). CIA-induced deficits were assayed by arthritic clinical scoring, paw thickness measurements, and behavioral tests of pain and paw function. Results: DEX or dual administration with JZL184 reduced paw thickness and clinical scores, and JZL184 dose-dependently attenuated grip strength and balance beam deficits caused by CIA. Traditional measures of pain-induced behaviors (hyperalgesia and allodynia) were inconsistent. The antiarthritic effects of JZL184 (40 mg/kg) were largely blocked by coadministration of the CB2 antagonist SR144528, and the DAGLβ inhibitor KT109 had no effect on CIA, indicating that these effects likely occurred through CB2 activation. Conclusions: MAGL inhibition reduced paw inflammation and pain-depressed behavioral signs of arthritis, likely through an endocannabinoid mechanism requiring CB2. These data support the development of MAGL as a target for therapeutic treatment of inflammatory arthritis.