PF-03382792
Based on 1 Customer Validation
PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 1400811-63-3
- Formula: C23H32FN3O4
- Molecular Weight:433.52
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All 5-HT Receptor Isoforms
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Biological Activity
|
5-HT4d Receptor |
5-HT4d Receptor 2.7 nM (Ki) |
5-HT4d Receptor 0.9 nM (EC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.8 nM
Compound: 3
|
Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| HEK293 | EC50 |
0.9 nM
Compound: 3
|
Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| HEK293 | EC50 |
1.15 nM
Compound: 3
|
Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| HEK293 | EC50 |
1.2 nM
Compound: 3
|
Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| HEK293 | EC50 |
1.3 nM
Compound: 3
|
Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| HEK293 | EC50 |
1.52 nM
Compound: 3
|
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| HEK293 | EC50 |
2.15 nM
Compound: 3
|
Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
|
[PMID: 22974325] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1400811-63-3
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Appearance Solid
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Molecular Weight 433.52
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Formula C23H32FN3O4
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Color White to off-white
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SMILES
O=C(N1C(C(C)(C)C2=C1C=C(F)C=C2)=O)NCC3CCN(CC4(O)CCOCC4)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (269 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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)