DC Chemicals Limited
China
Product Name: Kelatorphan
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Kelatorphan
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

92175-57-0

92175-57-0 structure

92175-57-0 structure

Name: Kelatorphan
Chemical Name: (2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]propanoic acid
CAS Number: 92175-57-0
Molecular Formula: C₁₄H₁₈N₂O₅
Molecular Weight: 294.30300
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2017-12-15 21:36:48
Modify Date: 2024-01-09 10:32:38
Kelatorphan is a full inhibitor of enkephalin degrading enzymes.

Name	(2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]propanoic acid
Synonyms	kelatorphan L-Alanine,N-(4-(hydroxyamino)-1,4-dioxo-2-(phenylmethyl)butyl)-,(R) (3-(N-Hydroxy)carboxamido-2-benzylpropanoyl)alanine n-[(2r)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]-l-alanine

Description	Kelatorphan is a full inhibitor of enkephalin degrading enzymes.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
Target	Enkephalin degrading enzyme[1].
In Vivo	The administration of Kelatorphan alone (50 μg) could result in a strong increase of intact [3H]enkephalin content corresponding to 80±11% of total recovered radioactivity[2]. In normal awake rats, Kelatorphan (10±20 mg/kg i.v.) increases minute-volume. The increase in ventilation is due to a dose-dependent increase in breathing frequency. In arthritic rats Kelatorphan (20 mg/kg i.v.) increases ventilation and there is no significant difference between arthritic and non-arthritic rats. In pentobarbital-anesthetized rats, a slight (116%) but significant increase of respiration is also produced by Kelatorphan (20 mg/kg, n=6) 10±15 min after administration. The effects of Kelatorphan are not antagonized by a pretreatment with a small dose of naloxone (0.2 mg/kg i.v., 15 min before Kelatorphan), but a larger dose (1 mg/kg) significantly antagonized Kelatorphan (20 mg/kg) at 5 and 10 min in awake rats[3].
References	[1]. Waksman G, et al. Kelatorphan: a full inhibitor of enkephalin degrading enzymes. Biochemical and pharmacological properties, regional distribution of enkephalinase in rat brain by use of a tritiated derivative. Neuropeptides. 1985 Feb;5(4-6):529-32. [2]. Waksman G, et al. In vitro and in vivo effects of kelatorphan on enkephalin metabolism in rodent brain. Eur J Pharmacol. 1985 Nov 5;117(2):233-43. [3]. Boudinot E, et al. Effects of the potent analgesic enkephalin-catabolizing enzyme inhibitors RB101 and kelatorphan on respiration. Pain. 2001 Feb 1;90(1-2):7-13.

Density	1.301g/cm3
Molecular Formula	C₁₄H₁₈N₂O₅
Molecular Weight	294.30300
Exact Mass	294.12200
PSA	115.73000
LogP	1.11190
Index of Refraction	1.567

Hazard Codes	Xi