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LGD-6972 Sale

目录号 : GC31343

LGD-6972是一种胰高血糖素受体拮抗剂。

LGD-6972 Chemical Structure

Cas No.:1207989-09-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,583.00
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1mg
¥994.00
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5mg
¥2,610.00
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10mg
¥4,230.00
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50mg
¥12,248.00
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100mg
¥18,208.00
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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

LGD-6972 is a glucagon receptor antagonist.

LGD-6972 has linear plasma pharmacokinetics consistent with once daily dosing that is comparable in healthy and T2DM subjects. Dose-dependent decreases in fasting plasma glucose are observed in all groups with a maximum of 3.15 mM (56.8 mg/dL) on day 14 in T2DM subjects. LGD-6972 also reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels decrease and insulin levels increase after an oral glucose load in T2DM subjects. LGD-6972 is well tolerated at the doses tested without dose-related or clinically meaningful changes in clinical laboratory parameters. No subject experiences hypoglycaemia[1].

[1]. Vajda EG, et al. Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2017 Jan;19(1):24-32.

Chemical Properties

Cas No. 1207989-09-0 SDF
Canonical SMILES O=C(NCCS(=O)(O)=O)C1=CC=C(C[C@H](C2=CC=C(C3=CC=C(C(C)(C)C)C=C3)C=C2)C(NC4=CC=C(C5=C(C)C=C(C)C=C5C)C=C4)=O)C=C1
分子式 C43H46N2O5S 分子量 702.9
溶解度 DMSO : ≥ 31 mg/mL (44.10 mM) 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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.4227 mL 7.1134 mL 14.2268 mL
5 mM 0.2845 mL 1.4227 mL 2.8454 mL
10 mM 0.1423 mL 0.7113 mL 1.4227 mL
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Research Update

Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus

Aim: To evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple doses of a novel, oral glucagon receptor antagonist, LGD-6972, in healthy subjects and subjects with type 2 diabetes (T2DM). Methods: In the single ascending dose study, LGD-6972 (2-480 mg) was administered to healthy subjects (n = 48) and T2DM subjects (n = 8). In the multiple ascending dose study, healthy subjects (n = 12) received a dose of 15 mg LGD-6972 and T2DM subjects (n = 36) received doses of 5, 10 or 15 mg of LGD-6972 daily for 14 days. Results: LGD-6972 had linear plasma pharmacokinetics consistent with once-daily dosing that was comparable in healthy and T2DM subjects. Dose-dependent decreases in fasting plasma glucose were observed in all groups with a maximum of 3.15 mmol/L (56.8 mg/dL) on day 14 in T2DM subjects. LGD-6972 also reduced plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon were observed, but glucagon levels decreased and insulin levels increased after an oral glucose load in T2DM subjects. LGD-6972 was well tolerated at the doses tested without dose-related or clinically meaningful changes in clinical laboratory parameters. No subject experienced hypoglycaemia. Conclusion: Inhibition of glucagon action by LGD-6972 was associated with decreases in glucose in both healthy and T2DM subjects, the magnitude of which was sufficient to predict improvement in glycaemic control with longer treatment duration in T2DM patients. The safety and pharmacological profile of LGD-6972 after 14 days of dosing supports continued clinical development.

Efficacy and Safety of the Glucagon Receptor Antagonist RVT-1502 in Type 2 Diabetes Uncontrolled on Metformin Monotherapy: A 12-Week Dose-Ranging Study

Objective: Evaluate the safety and efficacy of RVT-1502, a novel oral glucagon receptor antagonist, in subjects with type 2 diabetes inadequately controlled on metformin.
Research design and methods: In a phase 2, double-blind, randomized, placebo-controlled study, subjects with type 2 diabetes (n = 166) on a stable dose of metformin were randomized (1:1:1:1) to placebo or RVT-1502 5, 10, or 15 mg once daily for 12 weeks. The primary end point was change from baseline in HbA1c for each dose of RVT-1502 compared with placebo. Secondary end points included change from baseline in fasting plasma glucose (FPG) and safety assessments.
Results: Over 12 weeks, RVT-1502 significantly reduced HbA1c relative to placebo by 0.74%, 0.76%, and 1.05% in the 5-, 10-, and 15-mg groups (P < 0.001), respectively, and FPG decreased by 2.1, 2.2, and 2.6 mmol/L (P < 0.001). The proportions of subjects achieving an HbA1c <7.0% were 19.5%, 39.5%, 39.5%, and 45.0% with placebo and RVT-1502 5, 10, and 15 mg (P ≤ 0.02 vs. placebo). The frequency of hypoglycemia was low, and no episodes were severe. Mild increases in mean aminotransferase levels remaining below the upper limit of normal were observed with RVT-1502 but were reversible and did not appear to be dose related, with no other liver parameter changes. Weight and lipid changes were similar between RVT-1502 and placebo. RVT-1502-associated mild increases in blood pressure were not dose related or consistent across time.
Conclusions: Glucagon receptor antagonism with RVT-1502 significantly lowers HbA1c and FPG, with a safety profile that supports further clinical development with longer-duration studies (NCT02851849).