Difelikefalin - CAS 1024828-77-0
Catalog number:
1024828-77-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C36H53N7O6
Molecular Weight:
679.86
COA:
Inquire
Targets:
Opioid Receptor
Description:
Difelikefalin is an analgesic opioid peptide acting as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR). It acts as an analgesic by activating KORs on peripheral nerve terminals and KORs expressed by certain immune system cells. It may be useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. It is under development by Cara Therapeutics as an intravenous agent for the treatment of postoperative pain. It lacks the central side effects due to its peripheral selectivity. It is also being investigated for the treatment of pruritus (itching). It has completed phase II clinical trials for postoperative pain and has demonstrated significant and "robust" clinical efficacy, along with being safe and well-tolerated. It is also in phase II clinical trials for uremic pruritus in hemodialysis patients.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98 %
Appearance:
Solid powder
Synonyms:
CR845;CR-845;MR-13A-9;1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-aminopiperidine-4-carboxylic acid;4-Amino-1-[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Difelikefalin may be useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. It is used as an intravenous agent for the treatment of postoperative pain. It is also being investigated for the treatment of pruritus (itching).
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
1005.5±65.0 °C | Condition: Press: 760 Torr
Density:
1.214±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
FWMNVWWHGCHHJJ-SKKKGAJSSA-N
InChI:
InChI=1S/C36H53N7O6/c1-24(2)21-29(32(45)40-28(15-9-10-18-37)34(47)43-19-16-36(39,17-20-43)35(48)49)42-33(46)30(23-26-13-7-4-8-14-26)41-31(44)27(38)22-25-11-5-3-6-12-25/h3-8,11-14,24,27-30H,9-10,15-23,37-39H2,1-2H3,(H,40,45)(H,41,44)(H,42,46)(H,48,49)/t27-
Canonical SMILES:
CC(C)CC(C(=O)NC(CCCCN)C(=O)N1CCC(CC1)(C(=O)O)N)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC3=CC=CC=C3)N
Current Developer:
Difelikefalin is under development by Cara Therapeutics. It has completed phase II clinical trials for postoperative pain. It is also in phase II clinical trials for uremic pruritus in hemodialysis patients.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Opioid Receptor Products


CAS 1174130-61-0 LY-2456302

LY-2456302
(CAS: 1174130-61-0)

LY-2456302, also called as CERC-501, is a potent, highly selective and centrally-penetrant kappa opioid receptor antagonist(Ki= 0.807 nM)with favorable pharmaco...

CAS 1401031-39-7 TRV130 HCl

TRV130 HCl
(CAS: 1401031-39-7)

TRV130 is an opioid drug that is under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid recep...

LY 106737
(CAS: 82970-72-7)

LY 106737 is phenylpiperidine opioid receptor antagonist, but no detailed information has been published yet.

CAS 122752-16-3 Deltorphin 2

Deltorphin 2
(CAS: 122752-16-3)

Deltorphin 2, an anion transporting peptid, is a selective peptide agonist for theδ opioid receptor.

LY-190388
(CAS: 105496-35-3)

LY-190388 is an μ receptor agonist. It is a penicillamine-containing enkephalin analog and has analgesia effect.

(+)-Igmesine hydrochloride
(CAS: 130152-35-1)

Igmesine is a selective σ1 receptor ligand (KD = 19.1 nM), with nearly no activity at σ2 receptors (IC50 > 1000 nM). It was developed by Pfizer. Igmesine inhibi...

Nalfurafine hydrochloride
(CAS: 152658-17-8)

Nalfurafine is a selective and centrally-penetrant κ-opioid receptor (KOR) agonist without significant activity on μ- and δ-opioid receptors. With antipruritic ...

CAS 20410-95-1 6 α-naloxol

6 α-naloxol
(CAS: 20410-95-1)

6 α-naloxol, a human metabolite of naloxone, is an opioid antagonist.

Enadoline hydrochloride
(CAS: 124439-07-2)

Enadolineis a potent selective Opioid kappa receptor agonists originated by Pfizer. However, clinical trials for the treatment of Arrhythmias, Neuroprotection a...

CAS 59263-76-2 Meptazinol Hydrochloride

Meptazinol Hydrochloride
(CAS: 59263-76-2)

Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]-dihydromorphine binding with IC50 of 58 nM.

CAS 1108147-88-1 MCOPPB triHydrochloride

MCOPPB triHydrochloride
(CAS: 1108147-88-1)

The trihydrochloride salt form of MCOPPB, an effective full agonist of nociceptin receptor, could be a good antianxiety agent with few side-effects. pKi: 10.07.

CAS 152-02-3 Levallorphan

Levallorphan
(CAS: 152-02-3)

Levallorphan, an allylmorphinan derivative, has been found to be a μ-opioid receptor antagonist that could be an analgesic agent as an prescription drug.

CAS 156053-89-3 Alvimopan

Alvimopan
(CAS: 156053-89-3)

Alvimopan is a novel, oral, peripherally acting antagonist of the mu opioid receptor, which can help gastrointestinal recovery after surgery. Phase III IC50: Mu...

CHIR 4531
(CAS: 158198-48-2)

CHIR 4531, an oligopeptides compound, has been found to be an opioid mu receptor agonist and was once studied in pain therapy.

PD-117302
(CAS: 111728-01-9)

PD-117302, a new nonpeptide opioid compound, is a selective kappa-opioid agonist. It has been evaluated in vivo for antinociceptive activity and other effects c...

CAS 34140-59-5 Trimebutine Maleate

Trimebutine Maleate
(CAS: 34140-59-5)

Trimebutine is an opioid receptor agonist used as spasmolytic agent abdominal pain.

LY2795050
(CAS: 1346133-08-1)

LY2795050, a κ-opioid Receptor antagonist, has been found to be effective in imaging KOR behaving as a PET tracer. IC50: 0.72 nM and 25.8 nM for κ-opioid Recept...

CAS 152685-85-3 Hemorphin-7

Hemorphin-7
(CAS: 152685-85-3)

Hemorphin-7, a hemorphin peptide with antinociceptive and antihypertensive effects, is an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemo...

CAS 1354744-91-4 Naloxegol oxalate

Naloxegol oxalate
(CAS: 1354744-91-4)

Naloxegol oxalate is a CYP3A4 enzyme inhibitor, is a peripherally-selective opioid antagonist, for the treatment of opioid-induced constipation.

CAS 785835-79-2 JDTic dihydrochloride

JDTic dihydrochloride
(CAS: 785835-79-2)

JDTic dihydrochloride is a highly selective antagonist for the κ-opioid receptor with IC50 value of 0.02nM without affecting the μ- or δ-opioid receptors. It is...

Quick Inquiry

Verification code

Featured Items