CP-99994 hydrochloride
CP-99994 hydrochloride is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 hydrochloride prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 hydrochloride 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.
For research use only. We do not sell to patients.
- CAS No.: 145148-39-6
- Formula: C19H26Cl2N2O
- Molecular Weight:369.33
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Endogenous Metabolite Isoforms
More
Biological Activity
|
NK1R 0.25 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.5 nM
Compound: 1
|
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
|
10.1016/0960-894X(95)00220-N |
| CHO | IC50 |
0.5 nM
Compound: 3
|
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
|
[PMID: 8627597] |
| CHO | IC50 |
0.5 nM
Compound: CP-99994
|
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.
|
[PMID: 7535362] |
| CHO | IC50 |
0.5 nM
Compound: CP-99994
|
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
|
[PMID: 8709125] |
| CHO | IC50 |
0.6 nM
Compound: CP-99994
|
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
|
10.1016/0960-894X(95)00009-I |
| IM-9 | IC50 |
0.2 nM
Compound: CP-99994
|
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
|
[PMID: 7543579] |
| IM-9 | IC50 |
0.49 nM
Compound: 1, (CP-99994)
|
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
|
[PMID: 9871670] |
| IM-9 | IC50 |
0.63 nM
Compound: CP-99994
|
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
|
[PMID: 17967540] |
Chemical Information
-
CAS No. 145148-39-6
-
Molecular Weight 369.33
-
Formula C19H26Cl2N2O
-
SMILES
COC(C=CC=C1)=C1CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2.Cl.Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP-99994 hydrochloride Related Classifications
HY-12145 Related Classifications
Powered by Bioz