1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. Amylin Receptor Calcium Channel
  3. Eloralintide sodium

Eloralintide sodium  (Synonyms: LY-3841136 sodium)

Cat. No.: HY-P10798A Purity: 99.72%
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Eloralintide sodium is an Amylin Receptor agonist. Eloralintide sodium selectively activates AMY1R and AMY3R in cells expressing human or rat AMY1R, AMY3R or CTR. Eloralintide sodium activates AMYRs and CTR in rats, inducing a sustained decrease in plasma Ca2+ levels. Eloralintide sodium reduces appetite and body weight in both lean and obese rats. Eloralintide sodium can be used for research related to obesity.

For research use only. We do not sell to patients.

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Eloralintide sodium

Eloralintide sodium Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

Eloralintide sodium is an Amylin Receptor agonist. Eloralintide sodium selectively activates AMY1R and AMY3R in cells expressing human or rat AMY1R, AMY3R or CTR. Eloralintide sodium activates AMYRs and CTR in rats, inducing a sustained decrease in plasma Ca2+ levels. Eloralintide sodium reduces appetite and body weight in both lean and obese rats. Eloralintide sodium can be used for research related to obesity[1][2][3].

In Vitro

Eloralintide selectively activates AMY1R and AMY3R in UMUC3 cells expressing human or rat AMY1R, AMY3R or CTR, with an EC50 of 23.9 pM and a Ki of 478.1 pM for human AMY1R, an EC50 of 5.4 pM and a Ki of 48.1 pM for rat AMY1R, as well as an EC50 of 13.8 pM and a Ki of 161.0 pM for rat AMY3R[3].

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

Parmacokinetics
Species Dose Route AUC0-∞ Cmax Tmax T1/2 CL/F
Rat[3] 30 nmol/Kg s.c. 14182 nM·h 146 nM 24 52.8 h 2.1 mL/h/kg
Monkey[3] 20 nmol/Kg s.c. 35037 nM·h 135 nM 64 159 h 0.58 mL/h/kg
In Vivo

Eloralintide sodium (10-30 nmol/kg, s.c., single) activates AMYRs and CTR in rats, and induces a sustained decrease in plasma Ca2+ levels[1].
Eloralintide sodium (0.1-300 nmol/kg; s.c.; single dose) reduces food intake and body weight in lean rats, attenuates the induced conditioned taste aversion, and has an ED50 of 8.9 nmol/kg for reducing sweetener preference[3].
Eloralintide sodium (0.1-100 nmol/kg; s.c.; once every three days; 13 days) reduces food intake and body weight in male DIO rats by decreasing fat mass[3].

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

Animal Model: Rat[1]
Dosage: 10 or 30 nmol/kg
Administration: s.c.; single dose
Result: Induced a prolonged decrease in Ca2+ plasma levels.
Animal Model: Sprague-Dawley Rats (male, lean)[3]
Dosage: 0.1, 0.3, 1, 30, 100, 300 nmol/kg
Administration: s.c.; single dose
Result: Dose-dependently reduced food intake and body
weight, with an ED50 of 3.7 nmol/kg for 96-hour food intake reduction and a 14.9% body weight reduction at the 300 nmol/kg single dose.
Attenuated the induced conditioned taste avoidance.
Reached an ED50 of 8.9 nmol/kg for saccharin preference reduction.
Animal Model: Long Evans DIO SD Rat (male, diet-induced obese)[3]
Dosage: 0.1, 0.3, 1, 30, 100 nmol/kg
Administration: s.c.; every three days; 13 days
Result: Reduced food intake and body weight in a dose-dependent manner.
Reached an ED50 of 3.7 nmol/kg for change from baseline in food intake at 96 h.
Reached an ED50 of 6.1 nmol/kg for change from baseline in body weight at 96 h.
Resulted in fat mass loss accounting for approximately 85%, 77%, and 68% of total body weight loss at doses of 10, 30, and 100 nmol/kg Q3D, respectively.\nReached an ED50 of 0.8 nmol/kg for loss of fat mass.
Molecular Weight

4526.10 (free base)

Formula

C201H319N49O65S2.xNa

Appearance

Solid

Color

White to off-white

Sequence

{γGlu}-Cys-Asn-Thr-Ala-Thr-Cys-Ala-Thr-Gly-{Orn}-Leu-Ala-Glu-{(α-Me-Phe)}-Leu-Val-Arg-Ser-Ser-Asn-{(N-Me-Asn)}-Phe-Gly-Pro-{Lys(γGlu-γGlu-C20 diacid)}-Leu-Pro-Pro-Thr-Glu-Val-Gly-Ser-Asn-Thr-Tyr-NH2 (Methylene bridge: Cys2-Cys7)

Sequence Shortening

{γGlu}-CNTATCATG-{Orn}-LAE-{(α-Me-Phe)}-LVRSSN-{(N-Me-Asn)}-FGP-{Lys(γGlu-γGlu-C20 diacid)}-LPPTEVGSNTY-NH2 (Methylene 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: 

H2O : 100 mg/mL (Need ultrasonic)

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.72%

References
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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.

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Product Name:
Eloralintide sodium
Cat. No.:
HY-P10798A
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