ADX71441

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

MedKoo CAT#: 571360

CAS#: 1207440-88-7

Description: 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

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ADX71441
CAS# 1207440-88-7
Instruction

Theoretical Analysis

MedKoo Cat#: 571360
Name: ADX71441
CAS#: 1207440-88-7
Chemical Formula: C19H15ClF2N4O4
Exact Mass: 436.08
Molecular Weight: 436.800
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 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: 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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.