GL64
Based on 1 Customer Validation
GL64 is a selective agonist of ADGRD1 (EC50 = 3.98 μM). GL64 has low selectivity for ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4 isoforms. GL64 activates ADGRD1 by mimicking the satchel sequence. GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway. GL64 effectively inhibits osteoclastogenesis and prevents bone loss both in vitro and in vivo. GL64 is useful in the study of osteoclast-related diseases.
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- Pureté: 98.80%
- CAS No.: 488801-10-1
- Formule: C27H19Cl3N2O2
- Masse moléculaire:509.81
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
GL64 (10 μM) stimulates CRE-luciferase activity by more than 1.5-fold in ADGRD1-overexpressing HEK293T cells[1].
GL64 (10 μM) increases CRE-luciferase and endogenous adenosine cAMP levels in wt MEFs but has no effect on Adgrd1−/− cells[1].
GL64 (0-100 μM) does not increase CRE-luciferase in HEK293T cells overexpressing adhesion GPCRs, such as ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4, and does not activate nonadhesion GPCRs, including GPR68, NPFFR1, GPR183, and GPRC5B[1].
GL64 has weak agonist activity against ADGRD1 (EC50 = 16.89 μM) in stachel peptide-treated in ADGRD1-overexpressing HEK293T cells[1].
GL64 (10 μM, 6 days) inhibits the differentiation of male WT bone marrow-derived macrophages (BMMs) into mature osteoclasts but has no effect on Adgrd1−/− BMMs[1].
GL64 (10 μM, 6 days) down-regulates the mRNA expression levels of Dc-stamp, Acp5, and Nfatc1, during male mouse osteoclast maturation in BMMs[1].
GL64 (30 μM) increases endogenous cAMP levels in male BMMs[1].
GL64 (10 μM, 2 days) reduces NFATC1 nuclear localization in BMMs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMMs
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Concentration:10 μM
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Incubation Time:6 days
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Result:Down-regulateed the mRNA expression levels of Dc-stamp, Acp5, and Nfatc1.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 26563 ng/mL | 6.27 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OVX-induced postmenopausal osteoporosis mice (twelve-week-old female C57BL/6J) model[1]
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Dosage:30 mg/kg
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Administration:i.p., once a day, 4 weeks
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Result:Rescued OVX-induced bone loss, increased BMD, BV/TV, and TB. N.
Inhibited OVX-induced TRAP expression and enzyme hyperactivity in femurs, reduced the osteoclast number and surface erosion, suppressed TRAP enzyme activity in the calvarias.
Chemical Information
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CAS No. 488801-10-1
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Appearance Solid
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Masse moléculaire 509.81
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Formule C27H19Cl3N2O2
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Color White to off-white
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SMILES
O=C1C2=CC=CC=C2NC(N1C3=CC=C(C=C3)Cl)C4=CC(OCC5=C(C=C(C=C5)Cl)Cl)=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (196.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.90 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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 and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 and light). 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 |
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| DMSO | 1 mM | 1.9615 mL | 9.8076 mL | 19.6152 mL | 49.0379 mL |
| 5 mM | 0.3923 mL | 1.9615 mL | 3.9230 mL | 9.8076 mL | |
| 10 mM | 0.1962 mL | 0.9808 mL | 1.9615 mL | 4.9038 mL | |
| 15 mM | 0.1308 mL | 0.6538 mL | 1.3077 mL | 3.2692 mL | |
| 20 mM | 0.0981 mL | 0.4904 mL | 0.9808 mL | 2.4519 mL | |
| 25 mM | 0.0785 mL | 0.3923 mL | 0.7846 mL | 1.9615 mL | |
| 30 mM | 0.0654 mL | 0.3269 mL | 0.6538 mL | 1.6346 mL | |
| 40 mM | 0.0490 mL | 0.2452 mL | 0.4904 mL | 1.2259 mL | |
| 50 mM | 0.0392 mL | 0.1962 mL | 0.3923 mL | 0.9808 mL | |
| 60 mM | 0.0327 mL | 0.1635 mL | 0.3269 mL | 0.8173 mL | |
| 80 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6130 mL | |
| 100 mM | 0.0196 mL | 0.0981 mL | 0.1962 mL | 0.4904 mL |
GL64 Related Classifications
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