CP-99994
CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.
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- No. CAS: 136982-36-0
- Fòrmula: C19H24N2O
- Peso molecular:296.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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NK1R 0.25 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.5 nM
Compound: 1
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Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells
Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells
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10.1016/0960-894X(95)00220-N |
| CHO | IC50 |
0.5 nM
Compound: 3
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Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells
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[PMID: 8627597] |
| CHO | IC50 |
0.5 nM
Compound: CP-99994
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Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.
Binding affinity against human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.
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[PMID: 7535362] |
| CHO | IC50 |
0.5 nM
Compound: CP-99994
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Displacement of [125 I]-Tyr8 SP from the cloned human Tachykinin receptor 1 expressed in CHO cells
Displacement of [125 I]-Tyr8 SP from the cloned human Tachykinin receptor 1 expressed in CHO cells
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[PMID: 8709125] |
| CHO | IC50 |
0.6 nM
Compound: CP-99994
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Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells
Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells
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10.1016/0960-894X(95)00009-I |
| IM-9 | IC50 |
0.2 nM
Compound: CP-99994
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Inhibition of [125I]-BH-Substance P binding to tachykinin receptor 1 in human IM-9 cells
Inhibition of [125I]-BH-Substance P binding to tachykinin receptor 1 in human IM-9 cells
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[PMID: 7543579] |
| IM-9 | IC50 |
0.49 nM
Compound: 1, (CP-99994)
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Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells
Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells
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[PMID: 9871670] |
| IM-9 | IC50 |
0.63 nM
Compound: CP-99994
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Displacement of [3H]substance P from NK1 human receptor expressed in IM9 cells
Displacement of [3H]substance P from NK1 human receptor expressed in IM9 cells
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[PMID: 17967540] |
Chemical Information
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No. CAS 136982-36-0
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Peso molecular 296.41
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Fòrmula C19H24N2O
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SMILES
COC(C=CC=C1)=C1CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP-99994 Related Classifications
HY-12144 Related Classifications
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