MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 571360 | Name: ADX71441

Description:

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

ADX71441 is a GABAB positive allosteric modulator (PAM). ADX71441 increases urinary latencies and reduces the number of urinary events and the total and average urinary volumes. ADX71441 completely inhibits the micturition reflex and induced overflow incontinence in five out of 10 animals. GABAB PAM has potential as a novel approach for the treatment of overactive bladder. It may also mitigate alcoholism and have analgesic effects in the bladder.

Chemical Structure

ADX71441
CAS#1207440-88-7

Theoretical Analysis

MedKoo Cat#: 571360

Name: ADX71441

CAS#: 1207440-88-7

Chemical Formula: C19H15ClF2N4O4

Exact Mass: 436.0750

Molecular Weight: 436.80

Elemental Analysis: C, 52.25; H, 3.46; Cl, 8.12; F, 8.70; N, 12.83; O, 14.65

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
No Data
Synonym
ADX71441; ADX 71441; ADX-71441
IUPAC/Chemical Name
N-(5-(4-(4-chloro-3-fluorobenzyl)-6-methoxy-3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl)-2-fluorophenyl)acetamide
InChi Key
BQDMEJYNGXEHSW-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H15ClF2N4O4/c1-10(27)23-16-8-12(4-6-14(16)21)26-19(29)25(18(28)17(24-26)30-2)9-11-3-5-13(20)15(22)7-11/h3-8H,9H2,1-2H3,(H,23,27)
SMILES Code
O=C(C(OC)=NN1C2=CC=C(F)C(NC(C)=O)=C2)N(CC3=CC=C(Cl)C(F)=C3)C1=O
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

Preparing Stock Solutions

The following data is based on the product molecular weight 436.80 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
1: Hwa LS, Kalinichev M, Haddouk H, Poli S, Miczek KA. Reduction of excessive alcohol drinking by a novel GABAB receptor positive allosteric modulator ADX71441 in mice. Psychopharmacology (Berl). 2014 Jan;231(2):333-43. doi: 10.1007/s00213-013-3245-z. Epub 2013 Aug 22. PubMed PMID: 23975038; PubMed Central PMCID: PMC3947346. 2: Kalinichev M, Palea S, Haddouk H, Royer-Urios I, Guilloteau V, Lluel P, Schneider M, Saporito M, Poli S. ADX71441, a novel, potent and selective positive allosteric modulator of the GABA(B) receptor, shows efficacy in rodent models of overactive bladder. Br J Pharmacol. 2014 Feb;171(4):995-1006. doi: 10.1111/bph.12517. PubMed PMID: 24224799; PubMed Central PMCID: PMC3925038. 3: Kannampalli P, Poli SM, Boléa C, Sengupta JN. Analgesic effect of ADX71441, a positive allosteric modulator (PAM) of GABA(B) receptor in a rat model of bladder pain. Neuropharmacology. 2017 Nov;126:1-11. doi: 10.1016/j.neuropharm.2017.08.023. Epub 2017 Aug 18. PubMed PMID: 28823612. 4: Kalinichev M, Girard F, Haddouk H, Rouillier M, Riguet E, Royer-Urios I, Mutel V, Lütjens R, Poli S. The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABA(B) receptor with a potential for treatment of anxiety, pain and spasticity. Neuropharmacology. 2017 Mar 1;114:34-47. doi: 10.1016/j.neuropharm.2016.11.016. Epub 2016 Nov 23. PubMed PMID: 27889489. 5: Hyland NP, Golubeva AV. GABA(B) receptors in the bladder and bowel: Therapeutic potential for positive allosteric modulators? Br J Pharmacol. 2014 Feb 12. doi: 10.1111/bph.12617. [Epub ahead of print] PubMed PMID: 24641323; PubMed Central PMCID: PMC4562517. 6: Augier E, Dulman RS, Damadzic R, Pilling A, Hamilton JP, Heilig M. The GABA(B) Positive Allosteric Modulator ADX71441 Attenuates Alcohol Self-Administration and Relapse to Alcohol Seeking in Rats. Neuropsychopharmacology. 2017 Aug;42(9):1789-1799. doi: 10.1038/npp.2017.53. Epub 2017 Mar 15. PubMed PMID: 28294133; PubMed Central PMCID: PMC5520784. 7: Kalinichev M, Donovan-Rodriguez T, Girard F, Haddouk H, Royer-Urios I, Schneider M, Bate ST, Marker C, Pomonis JD, Poli S. ADX71943 and ADX71441, novel positive allosteric modulators of the GABA(B) receptor with distinct central/peripheral profiles, show efficacy in the monosodium iodoacetate model of chronic osteoarthritis pain in the rat. Eur J Pharmacol. 2017 Jan 15;795:43-49. doi: 10.1016/j.ejphar.2016.11.056. Epub 2016 Dec 1. PubMed PMID: 27916555.