2. GPCR/G Protein Neuronal Signaling
  3. Amylin Receptor CGRP Receptor
  4. Davalintide

Davalintide 是一种 Amylin (HY-P1464) 模拟肽，具有强的效力和更长效的作用。Davalintide 是胰淀素受体 (amylin receptor) (IC50 = 0.04 nM)、降钙素受体 (calcitonin receptor) (IC50 = 0.06 nM) 以及降钙素相关肽受体 (CGRP receptor) (IC50 = 3.1 nM) 的高效激动剂。Davalintide 与 Amylin 在通过降钙素受体激活环磷酸腺苷生成方面具有更强的效力 (EC50 = 1.4 nM)。Davalintide 通过多种机制调节血糖和体重，例如延缓胃排空、抑制胰高血糖素分泌以及减少食物摄入等。Davalintide 可用于抗肥胖和抗糖尿病的研究。

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Custom Peptide Synthesis

Davalintide

Davalintide Chemical Structure

CAS No. : 863919-85-1

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Davalintide 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Davalintide is an Amylin (HY-P1464)-mimetic peptide with greater potency and longer-lasting effects. Davalintide is a potent agonist of amylin receptor (IC50 = 0.04 nM), calcitonin receptor (IC50 = 0.06 nM) and calcitonin related peptide receptor (CGRP receptor) (IC50 = 3.1 nM). Davalintide shows stronger potency to Amylin to activate cyclic AMP production through the calcitonin receptor (EC50 = 1.4 nM). Davalintide regulates blood sugar and weight through various mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and reducing food intake. Davalintide can be used for the studies of anti-obesity and anti-diabetes[1][2].

药代动力学
(Parmacokinetics)[2]
Species Dose Route Indicator value
Rat 0.2 mg/kg s.c. Tmax 20 min
Rat 0.2 mg/kg s.c. T1/2 26 min
Rat 0.2 mg/kg s.c. Cmax 64.085 ng/mL
Rat 0.2 mg/kg s.c. AUC0-24 43.368 ng·h/mL
Rat 0.2 mg/kg s.c. Plasma Concentration 0.127 ng/mL
体内研究
(In Vivo)

Davalintide (1.09-1087 μg/kg (小鼠)；5 μg/kg (大鼠)，腹腔注射，单剂量) 可抑制禁食小鼠和过量喂养大鼠的食物摄入，其疗效和作用持续时间均优于 Amylin[1]。
Davalintide (1-100 μg/kg，腹腔注射，单剂量) 在减少大鼠食物摄入量时不影响其自主活动，其对食欲的抑制作用并非由恶心或厌恶等不良反应介导[1]。
Davalintide (1-100 μg/kg，皮下注射，每日一次，持续输注 8 周) 可有效减少大鼠的食物摄入量和体重，其减重主要体现在脂肪减少上，同时保持瘦体重，其代谢益处远不止简单的限制食物摄入量[1]。
Davalintide (10 μg/kg，皮下注射，每日一次，持续输注4周) 显著降低大鼠总热量摄入，降低对高脂肪和美味食物的偏好，并促使大鼠选择标准饲料[1]。
Davalintide (10 μg/kg，腹腔注射，单次给药) 作用于脑干后级区，通过更持久地激活大鼠的下游神经通路来达到抑制肥胖的效果[1]。
Davalintide (10 μg/kg，皮下注射，单次给药) 显著抑制麻醉大鼠精氨酸刺激引起的胰高血糖素升高，且对胰高血糖素的抑制作用具有特异性[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Acute food intake inhibition experiment established in fasted overnight NIH Swiss mice (24-30 g) and overfed Sprague-Dawley (SD) rats (weighing 394-461 g)[1]
Dosage: 1.09-1087 μg/kg (mice); 5 μg/kg (rats)
Administration: Intraperitoneal injection (i.p.), single dose
Result: And Amylin both significantly and dose-dependently inhibited acute food intake (mice ED50: 87 μg/kg vs. Amylin 110 μg/kg)
Exhibited the duration of action significantly longer than that of Amylin (23 hours vs. 6 hours) in the experiment where obese rats were subjected to the dark cycle (the main feeding period).
Animal Model: Behavioral safety experiment established fasted Sprague-Dawley (SD) rats (weighing 325-425 g)[1]
Dosage: 1, 10, 100 μg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Dose-dependently and persistently reduced food intake and body weight (8-week ED50 = 1.2 μg/kg/day).
Significantly reduced the level of plasma triglycerides.
Animal Model: Continuous infusion experiment (metabolic effect) established in obese rats induced by diet (Levin or SD rats, ~464 g), maintained on a 32% high-fat diet[1]
Dosage: 1, 3, 10, 100 μg/kg
Administration: Subcutaneous injection (s.c.), once daily for 8 weeks
Result: Dose-dependently and persistently reduced food intake and body weight (8-week ED50 = 1.2 μg/kg/day).
Significantly reduced the level of plasma triglycerides.
Animal Model: Food preference experiment established in DIO rats (~ 515 g) provided with both standard feed and 32% high-fat feed for them to choose freely[1]
Dosage: 10 μg/kg
Administration: Subcutaneous injection (s.c.), once daily for 4 weeks
Result: Significantly reduced total calorie intake.
Significantly reduced the preference for high-fat and delicious foods, and prompted the animals to choose standard feed.
Animal Model: Energy metabolism experiment established in SD rats (~ 421 g), maintained on a 32% high-fat diet for 5 weeks[1]
Dosage: 30 μg/kg
Administration: Subcutaneous injection (s.c.), once daily for 4 weeks
Result: Exhibited the energy consumption (VO₂) of not different from that in the Vehicle group.
Slight but significant increased RQ values at the end of the second week.
Animal Model: Area postrema (AP) damage experiment established in SD rats (weighing 175-200 g) underwent AP lesion surgery or sham surgery, and the experiments were conducted several months after recovery[1]
Dosage: 10 μg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly reduced food intake in the sham operation group.
Completely eliminated the effect of suppressing appetite in the AP lesion group.
Animal Model: Neuronal activation (c-Fos expression) established in SD rats (400 g), maintained on a 32% high-fat diet[1]
Dosage: 10 μg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Activated the same neural pathways to Amylin, but its effects lasted longer.
Animal Model: Glucagon inhibition experiment established in starved SD rats (250-280 g) and SD rats (350-370 g)[2]
Dosage: 10 μg/kg
Administration: Subcutaneous injection (s.c.), single dose
Result: Significantly inhibited the glucagon secretion stimulated by arginine.
Was no difference in blood glucose and insulin levels during the clamp period.
分子量

3624.03

Formula

C152H248N50O49S2
CAS 号
Sequence

Lys-Cys-Asn-Thr-Ala-Thr-Cys-Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-Thr-Gly-Ser-Asn-Thr-Tyr-NH2 (disulfide bridge:Cys2-Cys7)
Sequence Shortening

KCNTATCVLGRLSQELHRLQTYPRTNTGSNTY-NH2 (disulfide bridge:Cys2-Cys7)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Davalintide 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Davalintide863919-85-1Amylin ReceptorCGRP ReceptorAMYRCalcitonin gene-related peptide receptorAC2307davalintideamylinfood intakebody weightarea postremaInhibitorinhibitorinhibit

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