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

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.

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Davalintide

Davalintide Chemical Structure

CAS No. : 863919-85-1

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Based on 1 publication(s) in Google Scholar

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Description

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].

Parmacokinetics
Species Dose Route Tmax T1/2 Cmax AUC0-24 Plasma Concentration
Rat[2] 0.2 mg/kg s.c. 20 min 26 min 64.085 ng/mL 43.368 ng·h/mL 0.127 ng/mL
In Vivo

Davalintide (1.09-1087 μg/kg (mice); 5 μg/kg (rats), i.p., single dose) inhibits the food intake of fasting mice and overfed rats, and its efficacy and duration of action were both superior to Amylin[1].
Davalintide (1-100 μg/kg, i.p., single dose) does not affect the autonomous activities when food intake is reduced in rats, and its inhibitory effect on appetite is not mediated by adverse reactions such as nausea or aversion[1].
Davalintide (1-100 μg/kg, s.c., once daily, continuous infusion for 8 weeks) effectively reduces rats food intake and body weight with the weight loss mainly specific to fat reduction, while lean body mass preserved, and it has metabolic benefits that go beyond simply restricting food intake[1].
Davalintide (10 μg/kg, s.c., once daily, continuous infusion for 4 weeks) significantly reduces total calorie intake, decreases the preference for high-fat and tasty foods, and prompts rats to choose the standard feed[1].
Davalintide (10 μg/kg, i.p., single dose) relies on the Area Postrema and achieves the effect of suppressing obesity by more persistently activating the downstream neural pathways in rats[1].
Davalintide (10 μg/kg, s.c., single dose) significantly inhibits the increase in glucagon caused by arginine stimulation in anesthetized rats, and the inhibitory effect on glucagon is specific[2].

MedChemExpress (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.
Molecular Weight

3624.03

Formula

C152H248N50O49S2
CAS No.
Appearance

Solid

Color

White to light yellow

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)
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (3.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2759 mL 1.3797 mL 2.7594 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.2759 mL 1.3797 mL 2.7594 mL 6.8984 mL
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Davalintide Related Classifications

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  • 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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