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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- Pureza: 98.80%
- No. CAS: 488801-10-1
- Fòrmula: C27H19Cl3N2O2
- Peso molecular:509.81
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Almacenamiento:
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)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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.
| Species | Dose | Route | Cmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 26563 ng/mL | 6.27 h |
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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No. CAS 488801-10-1
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Appearance Solid
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Peso molecular 509.81
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Pureza y Documentación
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Ficha de datos (274 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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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GL64 Related Classifications
HY-175232 Related Classifications
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