2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. Nuclear Factor of activated T Cells (NFAT) Endogenous Metabolite
  4. GL64

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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GL64

GL64 Chemical Structure

CAS No. : 488801-10-1

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GL64 Related Antibodies

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Description

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[1].

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.

GL64 Related Antibodies

RT-PCR[1]

Cell Line: BMMs
Concentration: 10 μM
Incubation Time: 6 days
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

GL64 (30 mg/kg, i.p., once a day, 4 weeks) rescues osteoclast hyperactivity and bone loss in Ovariectomy (OVX)-induced postmenopausal osteoporosis mice model[1].

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

Animal Model: OVX-induced postmenopausal osteoporosis mice (twelve-week-old female C57BL/6J) model[1]
Dosage: 30 mg/kg
Administration: i.p., once a day, 4 weeks
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.
Molecular Weight

509.81

Formula

C27H19Cl3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC=CC=C2NC(N1C3=CC=C(C=C3)Cl)C4=CC(OCC5=C(C=C(C=C5)Cl)Cl)=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Purity & Documentation
References
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GL64 Related Classifications

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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.

Keywords:

GL64488801-10-1GL 64GL-64Nuclear Factor of activated T Cells (NFAT)Endogenous MetaboliteAgonistHEK293T cellsBMMsOVX mice modelpostmenopausal osteoporosisInhibitorinhibitorinhibit

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