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Arbaclofen placarbil

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

Hodoodo CAT#: H319758

CAS#: 847353-30-4

Description: Arbaclofen placarbil, also known as XP19986, is GABA(B) receptor agonist. Arbaclofen placarbil is a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen. Arbaclofen placarbil decreases postprandial reflux in patients with gastroesophageal reflux disease.

Chemical Structure

Arbaclofen placarbil

CAS# 847353-30-4

Instruction

Theoretical Analysis

Hodoodo Cat#: H319758
Name: Arbaclofen placarbil
CAS#: 847353-30-4
Chemical Formula: C19H26ClNO6
Exact Mass: 399.14
Molecular Weight: 399.868
Elemental Analysis: C, 57.07; H, 6.55; Cl, 8.87; N, 3.50; O, 24.01

Price and Availability

Size	Price	Availability	Quantity
10mg	USD -2
25mg	USD -2
50mg	USD -2
100mg	USD -2
200mg	USD -2
500mg	USD -2
1g	USD -1
2g	USD -1
5g	USD -1
10g	USD -1
20g	USD -1
50g	USD -1
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. Hodoodo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: XP19986; XP-19986; XP 19986; Arbaclofen placarbil.

IUPAC/Chemical Name: (R)-3-(4-chlorophenyl)-4-((((S)-1-(isobutyryloxy)-2-methylpropoxy)carbonyl)amino)butanoic acid

InChi Key: JXTAALBWJQJLGN-KSSFIOAISA-N

InChi Code: InChI=1S/C19H26ClNO6/c1-11(2)17(24)26-18(12(3)4)27-19(25)21-10-14(9-16(22)23)13-5-7-15(20)8-6-13/h5-8,11-12,14,18H,9-10H2,1-4H3,(H,21,25)(H,22,23)/t14-,18-/m0/s1

SMILES Code: O=C(O)C[C@H](C1=CC=C(Cl)C=C1)CNC(O[C@H](OC(C(C)C)=O)C(C)C)=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, not in water

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 399.87 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.

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: Erickson CA, Veenstra-Vanderweele JM, Melmed RD, McCracken JT, Ginsberg LD, Sikich L, Scahill L, Cherubini M, Zarevics P, Walton-Bowen K, Carpenter RL, Bear MF, Wang PP, King BH. STX209 (arbaclofen) for autism spectrum disorders: an 8-week open-label study. J Autism Dev Disord. 2014 Apr;44(4):958-64. doi: 10.1007/s10803-013-1963-z. PubMed PMID: 24272415.

2: Vakil NB, Huff FJ, Cundy KC. Randomised clinical trial: arbaclofen placarbil in gastro-oesophageal reflux disease--insights into study design for transient lower sphincter relaxation inhibitors. Aliment Pharmacol Ther. 2013 Jul;38(2):107-17. doi: 10.1111/apt.12363. Epub 2013 May 30. PubMed PMID: 23721547.

3: Borthwick L. Adulthood: Life lessons. Nature. 2012 Nov 1;491(7422):S10-1. PubMed PMID: 23136653.

4: Healy A, Rush R, Ocain T. Fragile X syndrome: an update on developing treatment modalities. ACS Chem Neurosci. 2011 Aug 17;2(8):402-10. doi: 10.1021/cn200019z. Epub 2011 Mar 22. Review. PubMed PMID: 22860169; PubMed Central PMCID: PMC3369755.

5: van der Pol R, Benninga MA, Smout AJ. Emerging therapies for GERD. J Pediatr Gastroenterol Nutr. 2011 Dec;53 Suppl 2:S10-1. Review. PubMed PMID: 22235450.

6: Hagerman R, Lauterborn J, Au J, Berry-Kravis E. Fragile X syndrome and targeted treatment trials. Results Probl Cell Differ. 2012;54:297-335. doi: 10.1007/978-3-642-21649-7_17. Review. PubMed PMID: 22009360; PubMed Central PMCID: PMC4114775.

7: Nance PW, Huff FJ, Martinez-Arizala A, Ayyoub Z, Chen D, Bian A, Stamler D. Efficacy and safety study of arbaclofen placarbil in patients with spasticity due to spinal cord injury. Spinal Cord. 2011 Sep;49(9):974-80. doi: 10.1038/sc.2011.43. Epub 2011 May 17. PubMed PMID: 21577221.

8: Vakil NB, Huff FJ, Bian A, Jones DS, Stamler D. Arbaclofen placarbil in GERD: a randomized, double-blind, placebo-controlled study. Am J Gastroenterol. 2011 Aug;106(8):1427-38. doi: 10.1038/ajg.2011.121. Epub 2011 Apr 26. PubMed PMID: 21519360.

9: Storr MA. What is nonacid reflux disease? Can J Gastroenterol. 2011 Jan;25(1):35-8. PubMed PMID: 21258666; PubMed Central PMCID: PMC3027332.

10: Kim GH. Arbaclofen placarbil decreases reflux with good tolerability in patients with gastroesophageal reflux disease (am j gastroenterol 2010;105:1266-1275). J Neurogastroenterol Motil. 2010 Oct;16(4):444-5. doi: 10.5056/jnm.2010.16.4.444. Epub 2010 Oct 30. PubMed PMID: 21103431; PubMed Central PMCID: PMC2978402.

11: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010 Sep;32(7):517-48. doi: 10.1358/mf.2010.32.7.1549223. PubMed PMID: 21069103.

12: Froestl W. Chemistry and pharmacology of GABAB receptor ligands. Adv Pharmacol. 2010;58:19-62. doi: 10.1016/S1054-3589(10)58002-5. PubMed PMID: 20655477.

13: Johnson DA, Levy BH 3rd. Evolving drugs in gastroesophageal reflux disease: pharmacologic treatment beyond proton pump inhibitors. Expert Opin Pharmacother. 2010 Jun;11(9):1541-8. doi: 10.1517/14656566.2010.482932. Review. PubMed PMID: 20450445.

14: Gerson LB, Huff FJ, Hila A, Hirota WK, Reilley S, Agrawal A, Lal R, Luo W, Castell D. Arbaclofen placarbil decreases postprandial reflux in patients with gastroesophageal reflux disease. Am J Gastroenterol. 2010 Jun;105(6):1266-75. doi: 10.1038/ajg.2009.718. Epub 2009 Dec 29. PubMed PMID: 20040914.

15: Lal R, Sukbuntherng J, Tai EH, Upadhyay S, Yao F, Warren MS, Luo W, Bu L, Nguyen S, Zamora J, Peng G, Dias T, Bao Y, Ludwikow M, Phan T, Scheuerman RA, Yan H, Gao M, Wu QQ, Annamalai T, Raillard SP, Koller K, Gallop MA, Cundy KC. Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen. J Pharmacol Exp Ther. 2009 Sep;330(3):911-21. doi: 10.1124/jpet.108.149773. Epub 2009 Jun 5. PubMed PMID: 19502531.

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