WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H524764
CAS#: 193356-17-1 (HCl)
Description: CO-101244, also known as RO-63-1908 and PD-174494, is a novel, potent and selective antagonist of NR2B-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for NR1A/2B, NR1A/2A and NR1A/2C subunit combinations respectively). CO-101244 displays neuroprotective effects in vivo and in vitro.
Hodoodo Cat#: H524764
Name: CO101244 HCl
CAS#: 193356-17-1 (HCl)
Chemical Formula: C21H28ClNO3
Exact Mass: 0.00
Molecular Weight: 377.910
Elemental Analysis: C, 66.74; H, 7.47; Cl, 9.38; N, 3.71; O, 12.70
Related CAS #: 193359-26-1 (free base) 193356-17-1 (HCl)
Synonym: CO-101244 hydrochloride; CO-101244 HCl; CO-101244; CO101244; RO-63-1908; RO-63 1908; RO63-1908; PD-174494; PD 174494; PD174494;
IUPAC/Chemical Name: 1-[2-(4-Hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]-4-piperidinol hydrochloride
InChi Key: WFFZHKKSIDENAJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H27NO3.ClH/c1-17-2-4-18(5-3-17)16-21(24)10-12-22(13-11-21)14-15-25-20-8-6-19(23)7-9-20;/h2-9,23-24H,10-16H2,1H3;1H
SMILES Code: OC1(CC2=CC=C(C)C=C2)CCN(CCOC3=CC=C(O)C=C3)CC1.[H]Cl
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 377.91 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: |
1: Cai L, Liow JS, Morse CL, Telu S, Davies R, Frankland MP, Zoghbi SS, Cheng K, Hall MD, Innis RB, Pike VW. Evaluation of 11C-NR2B-SMe and Its Enantiomers as PET Radioligands for Imaging the NR2B Subunit Within the NMDA Receptor Complex in Rats. J Nucl Med. 2020 Aug;61(8):1212-1220. doi: 10.2967/jnumed.119.235143. Epub 2020 Jan 10. Erratum in: J Nucl Med. 2021 Aug 1;62(8):1176. PMID: 31924728; PMCID: PMC7413242.
2: Michel A, Downey P, Nicolas JM, Scheller D. Unprecedented therapeutic potential with a combination of A2A/NR2B receptor antagonists as observed in the 6-OHDA lesioned rat model of Parkinson's disease. PLoS One. 2014 Dec 16;9(12):e114086. doi: 10.1371/journal.pone.0114086. PMID: 25513815; PMCID: PMC4267740.
3: Peng HY, Chen GD, Tung KC, Chien YW, Lai CY, Hsieh MC, Chiu CH, Lai CH, Lee SD, Lin TB. Estrogen-dependent facilitation on spinal reflex potentiation involves the Cdk5/ERK1/2/NR2B cascade in anesthetized rats. Am J Physiol Endocrinol Metab. 2009 Aug;297(2):E416-26. doi: 10.1152/ajpendo.00129.2009. Epub 2009 Jun 16. PMID: 19531642.
4: Peng HY, Chen GD, Tung KC, Lai CY, Hsien MC, Chiu CH, Lu HT, Liao JM, Lee SD, Lin TB. Colon mustard oil instillation induced cross-organ reflex sensitization on the pelvic-urethra reflex activity in rats. Pain. 2009 Mar;142(1-2):75-88. doi: 10.1016/j.pain.2008.11.017. Epub 2009 Jan 23. PMID: 19167822.
5: Peng HY, Chang HM, Lee SD, Huang PC, Chen GD, Lai CH, Lai CY, Chiu CH, Tung KC, Lin TB. TRPV1 mediates the uterine capsaicin-induced NMDA NR2B-dependent cross-organ reflex sensitization in anesthetized rats. Am J Physiol Renal Physiol. 2008 Nov;295(5):F1324-35. doi: 10.1152/ajprenal.00126.2008. Epub 2008 Jul 16. PMID: 18632800.
6: Peng HY, Chang HM, Chang SY, Tung KC, Lee SD, Chou D, Lai CY, Chiu CH, Chen GD, Lin TB. Orexin-A modulates glutamatergic NMDA-dependent spinal reflex potentiation via inhibition of NR2B subunit. Am J Physiol Endocrinol Metab. 2008 Jul;295(1):E117-29. doi: 10.1152/ajpendo.90243.2008. Epub 2008 May 13. PMID: 18477704.
7: Kocsis P, Kovács G, Farkas S, Horváth C, Szombathelyi Z, Tarnawa I. NR2B receptors are involved in the mediation of spinal segmental reflex potentials but not in the cumulative motoneuronal depolarization in vitro. Brain Res Bull. 2004 Aug 30;64(2):133-8. doi: 10.1016/j.brainresbull.2004.06.002. PMID: 15342100.
8: Nagy J. Renaissance of NMDA receptor antagonists: do they have a role in the pharmacotherapy for alcoholism? IDrugs. 2004 Apr;7(4):339-50. PMID: 15057640.
9: Kohl BK, Dannhardt G. The NMDA receptor complex: a promising target for novel antiepileptic strategies. Curr Med Chem. 2001 Sep;8(11):1275-89. doi: 10.2174/0929867013372328. PMID: 11562266.
