JNJ-10258859

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MedKoo CAT#: 525299

CAS#: 374927-03-4

Description: JNJ-10258859 is a novel, potent, and selective phosphodiesterase type 5 inhibitor. JNJ-10258859 inhibits phosphodiesterase type 5 with a K(i) of 0.23 nM and displayed excellent selectivity versus phosphodiesterase types 1-4 (>/=22,000 fold compared to phosphodiesterase type 5). JNJ-10258859 could be a useful treatment for erectile dysfunction.


Chemical Structure

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JNJ-10258859
CAS# 374927-03-4

Theoretical Analysis

MedKoo Cat#: 525299
Name: JNJ-10258859
CAS#: 374927-03-4
Chemical Formula: C30H24N4O3
Exact Mass: 488.18
Molecular Weight: 488.540
Elemental Analysis: C, 73.76; H, 4.95; N, 11.47; O, 9.82

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 @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: JNJ-10258859; JNJ 10258859; JNJ10258859; UNII-4NPX9224XR.

IUPAC/Chemical Name: 9H-Pyrrolo(3,4-b)quinolin-9-one, 3-(2,3-dihydro-5-benzofuranyl)-1,2,3,4-tetrahydro-2-(5-(4-methoxyphenyl)-2-pyrimidinyl)-, (3R)-

InChi Key: MVMQGWXVSBNFLB-MUUNZHRXSA-N

InChi Code: InChI=1S/C30H24N4O3/c1-36-22-9-6-18(7-10-22)21-15-31-30(32-16-21)34-17-24-27(33-25-5-3-2-4-23(25)29(24)35)28(34)20-8-11-26-19(14-20)12-13-37-26/h2-11,14-16,28H,12-13,17H2,1H3,(H,33,35)/t28-/m1/s1

SMILES Code: O=C1C2=C([C@@H](C3=CC=C(OCC4)C4=C3)N(C5=NC=C(C6=CC=C(OC)C=C6)C=N5)C2)NC7=C1C=CC=C7

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 488.54 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: Qiu Y, Bhattacharjee S, Kraft P, John TM, Craig E, Haynes-Johnson D, Guan J, Jiang W, Macielag M, Sui Z, Clancy J, Lundeen S. Characterization of a novel phosphodiesterase type 5 inhibitor: JNJ-10258859. Eur J Pharmacol. 2003 Jul 4;472(1-2):73-80. PubMed PMID: 12860475.