Naltrindole HydrochlorideA δ opioid (DOR) receptor antagonist

Naltrindole Hydrochloride (CAS 111469-81-9)

Naltrindole Hydrochloride | CAS 111469-81-9 is rated 5.0 out of 5 by 1.
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Application: A δ opioid (DOR) receptor antagonist
CAS Number: 111469-81-9
Purity: ≥95%
Molecular Weight: 451.0
Molecular Formula: C26H26N2O3•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Naltrindole Hydrochloride is the hydrochloride salt preparation of Naltrindole, which is an apoptotic agent and an inhibitor of cell growth. Naltrindole has been shown to be a cell permeable, highly potent and selective antagonist of DOR(δ opioids). Mechanistic studies show that Naltrindole treatement reduces phosphorylation of threonine 308 and Akt/PKB on serine 473 in cells. By reducing phosphorylation of Akt/PKB, downstream effectors glycogen synthase kinase-3β and transcription factors such as AFX and FKHR are also reduced.


References

1. Portoghese, P.S., et al. 1991. J. Med. Chem. 34: 1715-1720. PMID: 1851846
2. Verborgh, C., et al. 1999. Pharmacol. Biochem. Behav. 63: 175-183. PMID: 10340539
3. Chen, Y.L., et al. 2004. Cancer Res. 64: 8723-8730. PMID: 15574783

Physical State :
Solid
Solubility :
Soluble in water (8 mg/ml), and methanol (4.5 mg/ml).
Storage :
Store at -20° C
Refractive Index :
n20D 1.80 (Predicted)
IC50 :
Growth of NCI-H69: IC50 = 25 µM; Growth of NCI-H345: IC50 = 40 µM; Growth of NCI-H510 : IC50 = 55 µM
Ki Data :
MOR-1: Ki= 3.8 nM; KOR-1: Ki= 332.7 nM; DOR-1: Ki= 31 pM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
PB9092200
PubChem CID :
16760573
MDL Number :
MFCD00069313
SMILES :
C1CC1CN2CC[C@]34[C@@H]5C6=C(C[C@]3(C2CC7=C4C(=C(C=C7)O)O5)O)C8=CC=CC=C8N6.Cl

Download SDS (MSDS)

Certificate of Analysis

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Naltrindole Hydrochloride  Product Citations

See how others have used Naltrindole Hydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23973647  Izquierdo, T. et al. 2013. Eur. J. Pharmacol. 718: 393-400.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Chen et al Chen et al. (PubMed ID 15574783) used Naltrindole Hydrochloride to induce cell death by reducing phosphorylation of Akt/PKB in small cell lung cancer cells. -SCBT Publication Review
Date published: 2015-03-19
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