WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124618
CAS#: N/A
Description: AD258 is a Sigma Receptor Ligand with Potent Antiallodynic Activity. AD258 exhibited negligible in vitro cellular toxicity and a high binding affinity to both SRs (KiS1R = 3.5 nM, KiS2R = 2.6 nM), but not for other pain-related targets, and exerted high potency in a model of capsaicininduced allodynia, reaching the maximum antiallodynic effect at very low doses (0.6−1.25 mg/kg). Functional activity experiments showed that S1R antagonism is needed for the effects of AD258 and that it did not induce motor impairment. In addition, AD258 exhibited a favorable pharmacokinetic profile.
Hodoodo Cat#: H124618
Name: AD258
CAS#: N/A
Chemical Formula: C22H25N3
Exact Mass: 331.20
Molecular Weight: 331.460
Elemental Analysis: C, 79.72; H, 7.60; N, 12.68
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Synonym: AD258; AD-258; AD 258
IUPAC/Chemical Name: 4-(7-phenethyl-2,7-diazaspiro[4.4]nonan-2-yl)benzonitrile
InChi Key: KURULBHGVNUVDX-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H25N3/c23-16-20-6-8-21(9-7-20)25-15-12-22(18-25)11-14-24(17-22)13-10-19-4-2-1-3-5-19/h1-9H,10-15,17-18H2
SMILES Code: N#CC1=CC=C(N2CC3(CN(CCC4=CC=CC=C4)CC3)CC2)C=C1
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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 331.46 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: |
Dichiara M, Ambrosio FA, Lee SM, Ruiz-Cantero MC, Lombino J, Coricello A, Costa G, Shah D, Costanzo G, Pasquinucci L, Son KN, Cosentino G, González-Cano R, Marrazzo A, Aakalu VK, Cobos EJ, Alcaro S, Amata E. Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity. J Med Chem. 2023 Aug 3. doi: 10.1021/acs.jmedchem.3c00959. Epub ahead of print. PMID: 37535861.