Nexopamil

    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H328009

CAS#: 136033-49-3

Description: Nexopamil, also known as LU-49938, a calcium channel antagonist and serotonin 2A receptor antagonist potentially for the treatment of angina pectoris. Nexopamil inhibits both 5-HT-induced mesangial cell contraction and proliferation by blocking 5-HT2 receptors and the voltage-operated Ca2+ channels.

Chemical Structure

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Nexopamil
CAS# 136033-49-3
Instruction

Theoretical Analysis

Hodoodo Cat#: H328009
Name: Nexopamil
CAS#: 136033-49-3
Chemical Formula: C24H40N2O3
Exact Mass: 404.30
Molecular Weight: 404.595
Elemental Analysis: C, 71.25; H, 9.97; N, 6.92; O, 11.86

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Nexopamil; LU-49938; LU 49938; LU49938.

IUPAC/Chemical Name: (2S)-5-(Hexylmethylamino)-2-isopropyl-2-(3,4,5-trimethoxyphenyl)valeronitrile

InChi Key: SKDZEFVVFACNLS-DEOSSOPVSA-N

InChi Code: InChI=1S/C24H40N2O3/c1-8-9-10-11-14-26(4)15-12-13-24(18-25,19(2)3)20-16-21(27-5)23(29-7)22(17-20)28-6/h16-17,19H,8-15H2,1-7H3/t24-/m0/s1

SMILES Code: N#C[C@](C1=CC(OC)=C(OC)C(OC)=C1)(C(C)C)CCCN(CCCCCC)C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 404.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Nearing BD, Hutter JJ, Verrier RL. Potent antifibrillatory effect of combined blockade of calcium channels and 5-HT2 receptors with nexopamil during myocardial ischemia and reperfusion in dogs: comparison to diltiazem. J Cardiovasc Pharmacol. 1996 Jun;27(6):777-87. PubMed PMID: 8761843.

2: Park SJ, Lee JJ, Kirchengast M, Boulanger CM, Vanhoutte PM. The combined 5-HT2 receptor and calcium channel inhibitor LU49938 restores endothelium dependent responses in the regenerated endothelium of the porcine coronary artery. Cardiovasc Res. 1995 Jan;29(1):95-101. PubMed PMID: 7895245.

3: Montero A, Rodríguez-López A, Reverte M, López-Novoa JM. The effect of LU-49938 (nexopamil) on the activation by serotonin of mesangial cells. Fundam Clin Pharmacol. 1995;9(2):175-80. PubMed PMID: 7628831.

4: Park SJ, Boulanger CM, Kirchengast M, Vanhoutte PM. Effects of the combined 5-hydroxytryptamine2 receptor and Ca2+ channel antagonist LU49938 on the responsiveness of isolated porcine coronary arteries with and without endothelium. J Cardiovasc Pharmacol. 1994 Sep;24(3):517-22. PubMed PMID: 7528308.

5: Hohlfeld T, Braun M, Strobach H, Schrör K. Protection of reperfused ischemic pig myocardium by nexopamil, a new combined Ca2+ and serotonin antagonist. J Cardiovasc Pharmacol. 1994 Jun;23(6):922-31. PubMed PMID: 7523784.

6: Kirchengast M, Rübsamen K, Lehmann HD. Inhibition by the combined Ca2+ and 5-HT2 receptor antagonist nexopamil (LU 49938) of intracoronary thrombus formation in a canine model of arterial stenosis and intimal damage. J Cardiovasc Pharmacol. 1993 Nov;22(5):687-94. PubMed PMID: 7506319.