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NLG802 Sale

目录号 : GC64955

NLG802 是 indoximod 的前药,indoximod 是一种口服活性的吲哚胺2,3-双加氧酶(IDO)抑制剂。

NLG802 Chemical Structure

Cas No.:2071683-99-1

规格 价格 库存 购买数量
5mg
¥1,440.00
现货
10mg
¥2,250.00
现货
25mg
¥4,950.00
现货
50mg
¥8,550.00
现货
100mg
¥13,950.00
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

NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.

[1]. Kumar S, et al. Discovery of indoximod prodrugs and characterization of clinical candidate NLG802. Eur J Med Chem. 2020 Jul 15;198:112373.

Chemical Properties

Cas No. 2071683-99-1 SDF Download SDF
分子式 C20H30ClN3O3 分子量 395.92
溶解度 DMSO : 250 mg/mL (631.44 mM; Need ultrasonic) 储存条件 4°C, away from moisture
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
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 2.5258 mL 12.6288 mL 25.2576 mL
5 mM 0.5052 mL 2.5258 mL 5.0515 mL
10 mM 0.2526 mL 1.2629 mL 2.5258 mL
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Research Update

Discovery of indoximod prodrugs and characterization of clinical candidate NLG802

Eur J Med Chem 2020 Jul 15;198:112373.PMID:32422549DOI:10.1016/j.ejmech.2020.112373

A series of different prodrugs of indoximod, including estesrs and peptide amides were synthesized with the aim of improving its oral bioavailability in humans. The pharmacokinetics of prodrugs that were stable in buffers, plasma and simulated gastric and intestinal fluids was first assessed in rats after oral dosing in solution or in capsule formulation. Two prodrugs that produced the highest exposure to indoximod in rats were further tested in Cynomolgus monkeys, a species in which indoximod has oral bioavailability of 6-10% and an equivalent dose-dependent exposure profile as humans. NLG802 was selected as the clinical development candidate after increasing oral bioavailability (>5-fold), Cmax (6.1-3.6 fold) and AUC (2.9-5.2 fold) in monkeys, compared to equivalent molar oral doses of indoximod. NLG802 is extensively absorbed and rapidly metabolized to indoximod in all species tested and shows a safe toxicological profile at the anticipated therapeutic doses. NLG802 markedly enhanced the anti-tumor responses of tumor-specific pmel-1 T cells in a melanoma tumor model. In conclusion, NLG802 is a prodrug of indoximod expected to increase clinical drug exposure to indoximod above the current achievable levels, thus increasing the possibility of therapeutic effects in a larger fraction of the target patient population.