2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. PNU-142633

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

For research use only. We do not sell to patients.

PNU-142633 Chemical Structure

PNU-142633 Chemical Structure

CAS No. : 187665-65-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 449 In-stock
Solution
10 mM * 1 mL in DMSO USD 449 In-stock
Solid
5 mg USD 603 In-stock
10 mg USD 965 Get quote
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Based on 1 publication(s) in Google Scholar

PNU-142633 Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy[1][2].

IC50 & Target[1]

5-HT1D Receptor

6 nM (Ki)

In Vitro

The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan[1].

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

PNU-142633 Related Antibodies
In Vivo

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds[1].

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

Animal Model: Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode[1]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration: Intravenous injection
Result: Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.
Molecular Weight

422.52

Formula

C24H30N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C2C(CCO[C@H]2CCN3CCN(C4=CC=C(C(N)=O)C=C4)CC3)=C1)NC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 42 mg/mL (99.40 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3668 mL 11.8338 mL 23.6675 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

COA (247 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3668 mL 11.8338 mL 23.6675 mL 59.1688 mL
5 mM 0.4734 mL 2.3668 mL 4.7335 mL 11.8338 mL
10 mM 0.2367 mL 1.1834 mL 2.3668 mL 5.9169 mL
15 mM 0.1578 mL 0.7889 mL 1.5778 mL 3.9446 mL
20 mM 0.1183 mL 0.5917 mL 1.1834 mL 2.9584 mL
25 mM 0.0947 mL 0.4734 mL 0.9467 mL 2.3668 mL
30 mM 0.0789 mL 0.3945 mL 0.7889 mL 1.9723 mL
40 mM 0.0592 mL 0.2958 mL 0.5917 mL 1.4792 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1834 mL
60 mM 0.0394 mL 0.1972 mL 0.3945 mL 0.9861 mL
80 mM 0.0296 mL 0.1479 mL 0.2958 mL 0.7396 mL
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PNU-142633 Related Classifications

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:

PNU-142633187665-65-2PNU142633PNU 1426335-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1Danti-migraineplasmaproteinextravasationInhibitorinhibitorinhibit

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