2. GPCR/G Protein
  3. GCGR
  4. LSN3318839

LSN3318839 is an orally active positive modulator of the glucagon-like peptide-1 receptor (GLP-1R). LSN3318839 can increase the secretion of insulin and has the effect of lowering blood sugar.

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

LSN3318839 Chemical Structure

LSN3318839 Chemical Structure

CAS No. : 2764704-18-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of LSN3318839:

LSN3318839 Related Antibodies

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Description

LSN3318839 is an orally active positive modulator of the glucagon-like peptide-1 receptor (GLP-1R). LSN3318839 can increase the secretion of insulin and has the effect of lowering blood sugar[1].

In Vitro

LSN3318839 (0-19 μM) enhances the potency and efficacy of GLP-1(9-36) in GLP-1R-expressed HEK293 cells, but does not affect the potency of GLP1(7-36)[1].
LSN3318839 (1-3 μM) significantly increases insulin secretion in combination with GLP-1 (9-36) in INS-1 832-3 cells with high glucose presence[1].

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

LSN3318839 Related Antibodies
In Vivo

LSN3318839 (10-30 mg/kg; Oral administration; Single dose) has a hypoglycemic effect in hyperglycemic mouse model, and the combined effect with Sitagliptin (HY-13749) is better[1].
Pharmacokinetic Analysis in mice, rats and dogs[1]

在小鼠，大鼠和狗中的药代动力学分析[1]

Species Route Dose (mg/kg) AUC (nM×hour) Cmax (nM) T1/2 (h) Vdss (L/kg) Cl (mL/min/kg) Tmax (h) % F
mouse i.v. 1 3640 1430 2.1 1.6 9.0 / /
mouse p.o. 3 7300 2040 1.6 / / 0.58 67
rat i.v. 1 859 1420 0.6 1.6 41.9 / /
rat p.o. 3 1160 183 2.9 / / 1.8 45
dog i.v. 1 1880 6780 0.6 0.3 18.5 / /

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

Animal Model: Glucose bolus treated GIPR KO mice[1]
Dosage: 10 or 30 mg/kg
Administration: Oral administration (p.o.); Single dose
Result: Significantly reduced glucose excursion with the 30 mg/kg dose.
Showed additive glucose lowering effect coadministered with Sitagliptin (HY-13749).
Molecular Weight

480.39

Formula

C26H23Cl2N3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C[C@H](C1=CC=CC=C1C2=NC=C3N=CN(C3=C2)[C@@H](C4=C(C(C5CC5)=CC=C4Cl)Cl)C)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (20.82 mM; ultrasonic and warming and heat to 60°C; 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 2.0816 mL 10.4082 mL 20.8164 mL
5 mM 0.4163 mL 2.0816 mL 4.1633 mL
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. 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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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.81%

SDS (251 KB)

COA (256 KB) HNMR (266 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
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. 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 2.0816 mL 10.4082 mL 20.8164 mL 52.0410 mL
5 mM 0.4163 mL 2.0816 mL 4.1633 mL 10.4082 mL
10 mM 0.2082 mL 1.0408 mL 2.0816 mL 5.2041 mL
15 mM 0.1388 mL 0.6939 mL 1.3878 mL 3.4694 mL
20 mM 0.1041 mL 0.5204 mL 1.0408 mL 2.6021 mL
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LSN3318839 Related Classifications

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:

LSN33188392764704-18-7LSN 3318839LSN-3318839GCGRGlucagon ReceptorGCGR ModulatorHyperglycemia modelInhibitorinhibitorinhibit

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