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MedKoo Cat#: 574976 | Name: Aptiganel hydrochloride
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Description:

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

Aptiganel hydrochloride is a noncompetitive NMDA antagonist that has neuroprotective effects and may be useful in the treatment of stroke.

Chemical Structure

Aptiganel hydrochloride
CAS#137160-11-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 574976

Name: Aptiganel hydrochloride

CAS#: 137160-11-3 (HCl)

Chemical Formula: C20H22ClN3

Exact Mass: 339.1502

Molecular Weight: 339.87

Elemental Analysis: C, 70.68; H, 6.52; Cl, 10.43; N, 12.36

Price and Availability

Size Price Availability Quantity
10mg USD 385.00 2 Weeks
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Related CAS #
137160-11-3 (HCl) 137159-92-3 (free base)
Synonym
Aptiganel hydrochloride; Aptiganel HCl; Cerestat HCl, Cerestat hydrochloride; CNS 1102 HCl; CNS1102 HCl; CNS-1102 HCl;
IUPAC/Chemical Name
1-(m-Ethylphenyl)-1-methyl-3-(1-naphthyl)guanidine monohydrochloride
InChi Key
CKAKVKWRMCAYJD-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H21N3.ClH/c1-3-15-8-6-11-17(14-15)23(2)20(21)22-19-13-7-10-16-9-4-5-12-18(16)19;/h4-14H,3H2,1-2H3,(H2,21,22);1H
SMILES Code
Cl.CCc1cccc(c1)N(C)C(=N)Nc2cccc3ccccc23
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
>3 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 339.87 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.

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: Albers GW, Goldstein LB, Hall D, Lesko LM; Aptiganel Acute Stroke Investigators. Aptiganel hydrochloride in acute ischemic stroke: a randomized controlled trial. JAMA. 2001 Dec 5;286(21):2673-82. doi: 10.1001/jama.286.21.2673. PMID: 11730442. 2: McBurney RN. Development of the NMDA ion-channel blocker, aptiganel hydrochloride, as a neuroprotective agent for acute CNS injury. Int Rev Neurobiol. 1997;40:173-95. doi: 10.1016/s0074-7742(08)60720-5. PMID: 8989621. 3: Dyker AG, Edwards KR, Fayad PB, Hormes JT, Lees KR. Safety and tolerability study of aptiganel hydrochloride in patients with an acute ischemic stroke. Stroke. 1999 Oct;30(10):2038-42. doi: 10.1161/01.str.30.10.2038. PMID: 10512904. 4: Kroppenstedt SN, Schneider GH, Thomale UW, Unterberg AW. Protective effects of aptiganel HCl (Cerestat) following controlled cortical impact injury in the rat. J Neurotrauma. 1998 Mar;15(3):191-7. doi: 10.1089/neu.1998.15.191. PMID: 9528919. 5: Kroppenstedt SN, Schneider GH, Thomale UW, Unterberg AW. Neuroprotective properties of aptiganel HCL (Cerestat) following controlled cortical impact injury. Acta Neurochir Suppl. 1998;71:114-6. doi: 10.1007/978-3-7091-6475-4_34. PMID: 9779160. 6: Muir KW, Grosset DG, Lees KR. Effects of prolonged infusions of the NMDA antagonist aptiganel hydrochloride (CNS 1102) in normal volunteers. Clin Neuropharmacol. 1997 Aug;20(4):311-21. doi: 10.1097/00002826-199708000-00003. PMID: 9260729. 7: Bokesch PM, Halpin DP, Ranger WR, Drummond-Webb JJ, Marchand JE, Bronson RT, Warner KG, Kream RM. Immediate-early gene expression in ovine brain after hypothermic circulatory arrest: effects of aptiganel. Ann Thorac Surg. 1997 Oct;64(4):1082-7; discussion 1088. doi: 10.1016/s0003-4975(97)00801-1. PMID: 9354532. 8: Lees KR. Cerestat and other NMDA antagonists in ischemic stroke. Neurology. 1997 Nov;49(5 Suppl 4):S66-9. doi: 10.1212/wnl.49.5_suppl_4.s66. PMID: 9371155. 9: Ikonomidou C, Turski L. Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? Lancet Neurol. 2002 Oct;1(6):383-6. doi: 10.1016/s1474-4422(02)00164-3. PMID: 12849400. 10: Prabhakar S, Das CP. Ischaemic stroke: new frontiers. Neurol India. 1999 Sep;47(3):168-77. PMID: 10514574. 11: Bokesch PM, Seirafi PA, Warner KG, Marchand JE, Kream RM, Trapp B. Differential immediate-early gene expression in ovine brain after cardiopulmonary bypass and hypothermic circulatory arrest. Anesthesiology. 1998 Oct;89(4):961-8. doi: 10.1097/00000542-199810000-00021. PMID: 9778014. 12: Hoyte L, Barber PA, Buchan AM, Hill MD. The rise and fall of NMDA antagonists for ischemic stroke. Curr Mol Med. 2004 Mar;4(2):131-6. doi: 10.2174/1566524043479248. PMID: 15032709. 13: Muir KW, Lees KR. Excitatory amino acid antagonists for acute stroke. Cochrane Database Syst Rev. 2003;2003(3):CD001244. doi: 10.1002/14651858.CD001244. PMID: 12917902; PMCID: PMC7027997. 14: Muir KW, Lees KR. Clinical experience with excitatory amino acid antagonist drugs. Stroke. 1995 Mar;26(3):503-13. doi: 10.1161/01.str.26.3.503. PMID: 7886734. 15: Akins PT, Atkinson RP. Glutamate AMPA receptor antagonist treatment for ischaemic stroke. Curr Med Res Opin. 2002;18 Suppl 2:s9-13. doi: 10.1185/030079902125000660. PMID: 12365832. 16: Becker KJ, Tirschwell DL. Ensuring patient safety in clinical trials for treatment of acute stroke. JAMA. 2001 Dec 5;286(21):2718-9. doi: 10.1001/jama.286.21.2718. PMID: 11730448. 17: Muir KW, Grosset DG, Lees KR. Clinical pharmacology of CNS 1102 in volunteers. Ann N Y Acad Sci. 1995 Sep 15;765:279-89; discussion 298. doi: 10.1111/j.1749-6632.1995.tb16585.x. PMID: 7486614. 18: Sareen D. Neuroprotective agents in acute ischemic stroke. J Assoc Physicians India. 2002 Feb;50:250-8. PMID: 12038658. 19: Zhang R, Ding Y. Identification of Key Features of CNS Drugs Based on SVM and Greedy Algorithm. Curr Comput Aided Drug Des. 2020;16(6):725-733. doi: 10.2174/1573409915666191212095340. PMID: 31830888. 20: Hu LY, Guo J, Magar SS, Fischer JB, Burke-Howie KJ, Durant GJ. Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers. J Med Chem. 1997 Dec 19;40(26):4281-9. doi: 10.1021/jm970459c. Erratum in: J Med Chem 1998 Mar 12;41(6):1006. PMID: 9435897.