[bAla8]-Neurokinin A(4-10) - CAS 122063-01-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C35H56N8O10S
Molecular Weight:
780.93
COA:
Inquire
Targets:
Neurokinin Receptor
Description:
An agonist of neurokinin 2 (NK2) receptor
Sequence:
DSFVXLM
Synonyms:
H-Asp-Ser-Phe-Val-bAla-Leu-Met-NH2; DSFVXLM; L-alpha-aspartyl-L-seryl-L-phenylalanyl-L-valyl-beta-alanyl-L-leucyl-L-methioninamide; (3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[3-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-oxopropyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-oxobutanoic acid
Solubility:
DMSO
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
1236.1±65.0 ℃ at 760 Torr
Density:
1.265±0.06 g/cm3
InChIKey:
CKNPSJOMUQBPLA-WTWMNNMUSA-N
InChI:
1S/C35H56N8O10S/c1-19(2)15-24(32(50)40-23(30(37)48)12-14-54-5)39-27(45)11-13-38-35(53)29(20(3)4)43-33(51)25(16-21-9-7-6-8-10-21)41-34(52)26(18-44)42-31(49)22(36)17-28(46)47/h6-10,19-20,22-26,29,44H,11-18,36H2,1-5H3,(H2,37,48)(H,38,53)(H,39,45)(H,40,50)(H,41,52)(H,42,49)(H,43,51)(H,46,47)/t22-,23-,24-,25-,26-,29-/m0/s1
Canonical SMILES:
CC(C)CC(C(=O)NC(CCSC)C(=O)N)NC(=O)CCNC(=O)C(C(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C(CO)NC(=O)C(CC(=O)O)N
1.[3H][beta-Ala8]neurokinin A-(4-10): a novel, selective radioligand for the tachykinin NK2 receptor.
Goso C;Astolfi M;Parlani M;Manzini S Eur J Pharmacol. 1995 Dec 27;294(1):239-45.
The binding characteristics of the novel radioligand [3H][beta-Ala8]neurokinin A-(4-10) were assessed in hamster urinary bladder membranes. This labelled compound bound in a reversible, highly specific and concentration-dependent manner to a single class of high affinity binding sites with a Kd of 1.8 +/- 0.2 nM and a Bmax of 139 +/- 21 fmol/mg of protein. Specific binding of [3H][beta-Ala8]neurokinin A-(4-10) was displaced only by NK2, but not by NK1 or NK3, tachykinin receptor agonists and antagonists. Neurokinin A, [beta-Ala8]neurokinin A-(4-10), L 659877 [cyclo(Leu-Met-Gln-Trp-Phe-Gly)], MEN 10376 (H-Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Lys-NH2), MEN 10627 [cyclo(Met-Asp-Trp-Phe-Dap-Leu)cyclo(2 beta-5 beta)] and SR 48968 [(S)-N-methyl-N-[4-(4-acetylamino-4-phenylpiperidino)-2- (3,4-dichlorophenyl)butyl]benzamide] displaced the binding with Ki values of 0.4 +/- 0.1 nM, 1.9 +/- 0.36 nM, 3.05 +/- 0.1 nM, 7.9 +/- 0.4 microM, 0.36 +/- 0.02 nM and 2.5 +/- 0.9 nM, respectively. Functional data, obtained in isolated hamster urinary bladder strips with the newly developed tachykinin NK2 receptor antagonists (MEN 10627 and SR 48968), showed a good agreement with binding data. This novel radioligand could represent a new useful tool for the assessment of tachykinin NK2 receptor antagonists.
2.Tachykinins mediate contraction of the human lower esophageal sphincter in vitro via activation of NK2 receptors.
Huber O;Bertrand C;Bunnett NW;Pellegrini CA;Nadel JA;Nakazato P;Debas HT;Geppetti P Eur J Pharmacol. 1993 Aug 3;239(1-3):103-9.
The contractile response to natural tachykinins and selective peptide agonists for tachykinin receptors was studied in strips of circular smooth muscle of human lower esophageal sphincter in vitro. The effects of phosphoramidon, which inhibits neutral endopeptidase (EC.3.4.24.11) and of the non-peptide compounds, SR 48968 and CP-96,345, which selectively block NK1 and NK2 receptors, respectively, were also investigated. Substance P, neurokinin A and neurokinin B produced a concentration-dependent contractile response. The rank order of potency was neurokinin A > neurokinin B > substance P. Phosphoramidon (1 microM) potentiated the response to substance P without changing the order of potency of natural tachykinins. The NK2-selective agonist, ([ beta Ala8]neurokinin A-(4-10)), produced a concentration-dependent contraction. The NK1 ([Sar9,Met(O2)11]substance P, 1 microM) and NK3 ([MePhe7]neurokinin B, 1 microM) selective agonists, however, did not exert any contractile effect. The selective NK2 antagonist, SR 48968, potently inhibited in a concentration-dependent (10 nM-1 microM) manner the response to neurokinin A, without affecting the response to carbachol. The selective NK1 antagonist, CP-96,345 (1 microM), did not affect the response to neurokinin A.
3.Inflammatory and motor responses by tachykinins in the guinea-pig oesophageal sphincter.
Conte B;Parlani M;Lopez G;Cirillo R;Maggi CA;Manzini S J Auton Pharmacol. 1998 Oct;18(5):313-7.
1. The aim of this study was to characterize the tachykinin receptors involved in producing plasma protein extravasation and contractile responses of the guinea-pig oesophageal sphincter. 2. In anaesthetized guinea-pigs, the selective tachykinin NK-1 receptor agonist [Sar9,Met(O2)11]substance P produced plasma protein extravasation (PPE) which was not affected by the treatment with the tachykinin NK-2 receptor antagonist MEN 10627 (1 micromol kg(-1) i.v.) or the histamine H1-receptor antagonist, diphenhydramine (34.5 micromol kg(-1) i.v.). However, the [Sar9,Met(O2)11]substance P-induced PPE was blocked by the previous administration of the peptide tachykinin NK-1 receptor antagonist FK 888 or by the non-peptide antagonist SR 140333, yielding ED50 values of 1.1 +/- 0.2 and 0.01 +/- 0.004 micromol kg(-1) i.v., respectively. 3. The tachykinin NK-2 or NK-3 receptor agonists [beta-Ala8]neurokinin A (4-10) or [MePhe7]neurokinin B, respectively, produced a weak PPE at high doses. The effect of [MePhe7]neurokinin B-induced PPE was inhibited by SR 140333. 4. In the guinea-pig isolated oesophageal sphincter, [Sar9,Met(O2)11]substance P did not exert any contractile effect up to 10 microM. The selective tachykinin NK-2 receptor agonist ([beta-Ala8]neurokinin A (4-10), produced concentration-dependent contractions (pD2 = 7.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Neurokinin Receptor Products


CAS 174635-53-1 SB 218795

SB 218795
(CAS: 174635-53-1)

SB 218795 is a potent and competitive non-peptide NK3 receptor antagonist (Ki = 13 nM at hNK3) displaying 90-fold and 7000-fold selectivity over hNK2 and hNK1 r...

CAS 172673-20-0 Fosaprepitant dimeglumine

Fosaprepitant dimeglumine
(CAS: 172673-20-0)

Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.

CAS 2990-43-4 Eledoisin-Related Peptide

Eledoisin-Related Peptide
(CAS: 2990-43-4)

Eledoisin-Related Peptide is a tachykinin receptor ligand.

CAS 214487-46-4 MEN11467

MEN11467
(CAS: 214487-46-4)

MEN11467, a pseudopeptide,is a new tachykinin NK1 receptor antagonist which potently antagonizes both tachykinin and antigen-mediated inflammatory responses of ...

CAS 137593-52-3 GR 64349

GR 64349
(CAS: 137593-52-3)

GR 64349 is a potent and selective agonist of tachykinin NK2 receptor (EC50 = 3.7 nM in rat colon).

CAS 86933-74-6 Neurokinin A

Neurokinin A
(CAS: 86933-74-6)

Neurokinin A is a member of the endogenous tachykinin agonist with preference for the NK-2R (NK-2 receptor).

CAS 135721-56-1 MDL 29913

MDL 29913
(CAS: 135721-56-1)

MDL 29913 is a selective NK2 tachykinin receptor antagonist which can be used in the treatment of IBS.

CAS 122063-01-8 [bAla8]-Neurokinin A(4-10)

[bAla8]-Neurokinin A(4-10)
(CAS: 122063-01-8)

An agonist of neurokinin 2 (NK2) receptor

CAS 188923-01-5 L760735

L760735
(CAS: 188923-01-5)

L760735 is a high-affinity NK1 receptor antagonist with IC50 value of 0.19 nM. It is selective over NK2 and NK3 receptors. It is used in the synthetic preparati...

CAS 264618-38-4 SSR 146977 hydrochloride

SSR 146977 hydrochloride
(CAS: 264618-38-4)

SSR 146977 hydrochloride is a potent and selective NK3 receptor antagonist (Ki = 0.26 and 19.3 nM in CHO cells expressing the human NK3 and NK2 receptor, respec...

CAS 148700-85-0 L-733,060

L-733,060
(CAS: 148700-85-0)

L-733,061, a phenylpiperidine derivative, has been found to be a NK1 receptor antagonist that could probably be antidepressant/ anxiolytic agent and also show a...

CAS 174636-32-9 SB 223412

SB 223412
(CAS: 174636-32-9)

SB 223412 is a brain penetrating and orally bioactive non-peptide NK3 receptor antagonist (Ki = 1, 144 and >100000 nM for human NK3, NK2 and NK1 receptors, resp...

CAS 170729-80-3 Aprepitant

Aprepitant
(CAS: 170729-80-3)

Aprepitant is a specific NK-1R antagonist, used as an antiemetic agent.

Talnetant hydrochloride
(CAS: 204519-66-4)

Talnetant is the hydrochloride salt of Talnetant. Talnetant, also called as SB 223412, is a selective, competitive, nonpeptide NK3 receptor antagonist and is in...

CAS 103222-11-3 RC 160

RC 160
(CAS: 103222-11-3)

RC 160 is a cyclic octapeptide somatostatin analog (Ki= 0.7, 5.4, 30.9, 45 and > 1000 nM for sst5, sst2, sst3, sst4 and sst1 receptors respectively). RC 160 is ...

CAS 174635-69-9 SB 222200

SB 222200
(CAS: 174635-69-9)

SB 222200 is a brain penetrating and non-peptide NK3 receptor antagonist (Ki = 4.4, > 100,000 and 250 nM for human NK3, NK1 and NK2 receptors, respectively) tha...

CAS 132746-60-2 CP 96345

CP 96345
(CAS: 132746-60-2)

CP 96345 is an effective and selective non-peptide NK1 receptor antagonist and has been found to show activities in restraining neurogenic inflammation in vivo.

CAS 914462-92-3 Rolapitant HCl hydrate

Rolapitant HCl hydrate
(CAS: 914462-92-3)

Rolapitant, also known as SCH-619734, is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist with potential antiemetic activity. Unl...

CAS 153050-21-6 SR 140333

SR 140333
(CAS: 153050-21-6)

SR 140333 is a potent NK1 receptor antagonist (Ki = 0.74 nM. IC50 = 1.6 nM). SR 140333 inhibits substance P-invoked calcium mobilization and outward current (IC...

CAS 148687-76-7 L-733,060 hydrochloride

L-733,060 hydrochloride
(CAS: 148687-76-7)

The hydrochloride salt form of L-733,061, a phenylpiperidine derivative, has been found to be a NK1 receptor antagonist that could probably be antidepressant/ a...

Chemical Structure

CAS 122063-01-8 [bAla8]-Neurokinin A(4-10)

Quick Inquiry

Verification code

Featured Items