2. GPCR/G Protein
  3. GCGR
  4. Orforglipron hemicalcium hydrate

Orforglipron hemicalcium hydrate  (Synonyms: LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate)

Cat. No.: HY-112185A Purity: 99.71%
SDS
COA
Handling Instructions Technical Support

Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete.

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

Orforglipron hemicalcium hydrate Chemical Structure

Orforglipron hemicalcium hydrate Chemical Structure

CAS No. : 3008544-96-2

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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 Orforglipron hemicalcium hydrate:

Orforglipron hemicalcium hydrate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Orforglipron hemicalcium hydrate

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete[1].

In Vivo

Orforglipron hemicalcium hydrate (0.94-4.8 nM in plasma concentration, i.v., or 0.05-0.1 mg/mL, i.g. for 5 days) suppresses food intake in a dose-dependent manner, promotes insulin secretion and blood glucose reduction in cynomolgus monkey model[1].
Orforglipron hemicalcium hydrate (0.05-1.35 mg/kg, i.g.) reaches Cmax 2 hours after administration at all doses, exhibits proportional ratio of increase in plasma drug exposure to dose increase, indicates a dose-dependent absorption in the gastrointestinal tract[1].

Pharmacokinetic Analysis of Orforglipron hemicalcium hydrate in cynomolgus monkey [1]

route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUC0-24h (ng·h/mL)
i.g. 0.05 2.0 4.78 23.7
i.g. 0.15 2.0 20.7 135
i.g. 0.45 2.0 32.0 208
i.g. 1.35 2.0 148 1040

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

Animal Model: cynomolgus monkey model[1]
Dosage: 0.9-4.8 nM; or 0.05-0.1 mg/mL
Administration: continuous i.v. administration for 30 minutes until a plasma concentration of 0.9-4.8 nM at steady state;
i.g. for 5 days with dose of 0.05-0.1 mg/mL
Result: Increased insulin secretion and decreased plasma-glucose.
Suppressed food intake in a dose-dependent manner.
Molecular Weight

921.02

Formula

C48H48F2N10O5.1/2Ca.H2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]1[C@](N2C3=CC=C([C@]4([H])CC(C)(OCC4)C)C=C3C=C2C(N5[C@H](C6=C(N7C(N(C8=CC=C(N(N=C9)C)C9=C8F)C=C7)=O)N(C%10=CC(C)=C(C(C)=C%10)F)N=C6CC5)C)=O)(C(N%11)=NOC%11=O)C1.[0.5].[Ca].O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (27.14 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 1.0858 mL 5.4288 mL 10.8575 mL
5 mM 0.2172 mL 1.0858 mL 2.1715 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 (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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.71%

SDS (252 KB)

COA (257 KB) HNMR (261 KB) LCMS (95 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 (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 1.0858 mL 5.4288 mL 10.8575 mL 27.1438 mL
5 mM 0.2172 mL 1.0858 mL 2.1715 mL 5.4288 mL
10 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7144 mL
15 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8096 mL
20 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL
25 mM 0.0434 mL 0.2172 mL 0.4343 mL 1.0858 mL
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Orforglipron hemicalcium hydrate 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:

Orforglipron hemicalcium3008544-96-2LY3502970 hemicalciumGLP-1 receptor agonist 1 hemicalciumGCGRGlucagon Receptortype 2 diabetecynomolgus monkeyInhibitorinhibitorinhibit

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