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MedKoo Cat#: 326896 | Name: Aptiganel

Description:

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

Aptiganel, also known as CNS-1102, and Cerestat; was a drug candidate that acted as a noncompetitive NMDA antagonist and that was under development by Cambridge Neuroscience, Inc as a treatment for stroke. It has neuroprotective effects and was researched for potential use in the treatment of stroke, but despite positive results in animal studies, human trials showed limited efficacy.

Chemical Structure

Aptiganel
CAS#137159-92-3 (free base)

Theoretical Analysis

MedKoo Cat#: 326896

Name: Aptiganel

CAS#: 137159-92-3 (free base)

Chemical Formula: C20H21N3

Exact Mass: 303.1735

Molecular Weight: 303.41

Elemental Analysis: C, 79.17; H, 6.98; N, 13.85

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.
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Related CAS #
137160-11-3 (HCl) 137159-92-3 (free base)
Synonym
CNS-1102; CNS 1102; CNS1102; Aptiganel; Cerestat.
IUPAC/Chemical Name
1-(3-ethylphenyl)-1-methyl-3-(naphthalen-1-yl)guanidine
InChi Key
BFNCJMURTMZBTE-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H21N3/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)
SMILES Code
N=C(NC1=C2C=CC=CC2=CC=C1)N(C3=CC=CC(CC)=C3)C
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 303.41 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. PubMed PMID: 11730442. 2: 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. PubMed PMID: 10512904. 3: 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. PubMed PMID: 9779160. 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. PubMed PMID: 9528919. 5: 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. PubMed PMID: 9354532. 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. PubMed PMID: 9260729. 7: 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. Review. PubMed PMID: 8989621.