AF-353


Catalog No. size PriceQuantity
M6717-2 2mg solid $108
M6717-10 10mg solid $447

Description

Cas:865305-30-2

Product Information

AF-353 is a P2X3 receptor antagonist. Antagonism of the P2X3 receptor is one of the potential therapeutic strategies for the management of neuropathic pain because P2X3 receptors are predominantly localized on small to medium diameter C- and Aδ-fiber primary afferent neurons, which are related to the pain-sensing system.

 

Chemical Formula: C14H17IN4O2

 

Exact Mass: 400.0396

 

Molecular Weight: 400.2205 

 

Elemental Analysis: C, 42.02; H, 4.28; I, 31.71; N, 14.00; O, 8.00

 

Synonym: 

 

AF353

AF-353

AF 353

 

Chemical Name:

5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine

 

InChi Key:

AATPYXMXFBBKFO-UHFFFAOYSA-N

 

InChi Code:  InChI=1S/C14H17IN4O2/c1-7(2)8-4-11(20-3)9(15)5-10(8)21-12-6-18-14(17)19-13(12)16/h4-7H,1-3H3,(H4,16,17,18,19)

 

Smiles Code:

NC1=NC=C(OC2=CC(I)=C(OC)C=C2C(C)C)C(N)=N1

 

 

Technical Data:

 

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

 

In Vitro

AF-353 (Ro-4) is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels.

AF-353 (Ro-4) also blocks human P2X2/3 channel function with marginally reduced potency with a p50 of 7.3.

 

In Vivo

AF-353 (Ro-4) does not compromise oxygen levels or cardiac function.

AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats.

AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced.

 

 

References

 

  1. Jung YH, Kim YO, Lin H, Cho JH, Park JH, Lee SD, Bae J, Kang KM, Kim YG, PaeAN, Ko H, Park CS, Yoon MH, Kim YC. Discovery of Potent Antiallodynic Agents for Neuropathic Pain Targeting P2X3 Receptors. ACS Chem Neurosci. 2017 Apr 6. doi:10.1021/acschemneuro.6b00401. [Epub ahead of print] PubMed PMID: 28323403.

 

Products are for research use only. Not for human use.

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