BI-9508
BI-9508 is a blood-brain barrier-penetrant GPR88 agonist. BI-9508 acts through activation of the Gi1 signaling pathway; it exists as atropisomers, with the more active isomer showing stronger agonist potency and lower P-glycoprotein efflux. BI-9508 can be used in GPR88-related central nervous system research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
The BI-9508 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- CAS. Nr.: 3082554-75-1
- Formel: C28H29F2N5O3
- Molecular Weight:521.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hGPR88 Gi1 BRET 47 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
47 nM
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Activation of human GPR88-mediated Gi1 BRET in HEK293 cells incubated 10 min with Prolume Purple as substrate.
Activation of human GPR88-mediated Gi1 BRET in HEK293 cells incubated 10 min with Prolume Purple as substrate.
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38949964 |
In Vitro
BI-9508 (compound 6) (100-0.003 μM; 10 min) has an hGPR88 Gi1 BRET EC50 of 47 nM in HEK293 cells, whereas the 6-Atro2 atropisomer has a significantly lower potency of 951 nM[1].
BI-9508 (100-0.003 μM; 10 min) has an mGPR88 Gi1 BRET EC50 of 94 nM in cells expressing mouse GPR88[1].
BI-9508 (1 μM; up to 2 h) has a PGP efflux ratio of 1.1 in MDCK-MDR1 cells[1].
BI-9508 (1 μM; 2 h at 37°C) binds to mouse plasma proteins at a rate of 99.1%[1].
The mouse liver microsome QH of BI-9508 (1 μM) is 40%[1].
BI-9508 has a high-throughput solubility of < 1 μg/mL at pH 7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BI-9508 (80 μmol/kg; i.p.; single dose) gives a Cunbound,30 of 2.83 nmol/L in male C57BL6/N mice; the doseEC50,30 is 108 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3082554-75-1
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Molecular Weight 521.56
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Formel C28H29F2N5O3
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SMILES
CC(C)OC1=CC=C(C2=C3C(N(C)N=C3)=C(N(CCOC(F)F)C([C@H]4[C@H](C5=CC=NC=N5)C4)=O)C=C2)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (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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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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