ICI 154,129

δ selective peptide antagonist CAS# 83420-94-4

ICI 154,129

Catalog No. BCC5677----Order now to get a substantial discount!

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ICI 154,129: 5mg $1139 In Stock
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Quality Control of ICI 154,129

Number of papers citing our products

Chemical structure

ICI 154,129

3D structure

Chemical Properties of ICI 154,129

Cas No. 83420-94-4 SDF Download SDF
PubChem ID 3035055 Appearance Powder
Formula C34H46N4O6S M.Wt 638.83
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 1 mg/ml in methanol
Sequence YGFL

(Modifications: Tyr-1 = N,N-diallyl-Tyr, Gly-2 - Phe-3 peptide bond replaced with Psi-(CH2S))

Chemical Name (2S)-2-[[(2S)-2-[2-[[2-[[(2S)-2-[bis(prop-2-enyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]ethylsulfanyl]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
SMILES CC(C)CC(C(=O)O)NC(=O)C(CC1=CC=CC=C1)SCCNC(=O)CNC(=O)C(CC2=CC=C(C=C2)O)N(CC=C)CC=C
Standard InChIKey CZRZYRKTYLLLRL-DTXPUJKBSA-N
Standard InChI InChI=1S/C34H46N4O6S/c1-5-17-38(18-6-2)29(21-26-12-14-27(39)15-13-26)32(41)36-23-31(40)35-16-19-45-30(22-25-10-8-7-9-11-25)33(42)37-28(34(43)44)20-24(3)4/h5-15,24,28-30,39H,1-2,16-23H2,3-4H3,(H,35,40)(H,36,41)(H,37,42)(H,43,44)/t28-,29-,30-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ICI 154,129

DescriptionSelective δ opioid antagonist.

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References on ICI 154,129

Ethological analyses of the effects of naloxone and the opiate antagonist ICI 154, 129 on social interactions in male house mice.[Pubmed:24897570]

Behav Processes. 1985 May;10(4):341-54.

The influences of the mu blocker naloxone and the novel opioid delta receptor antagonist ICI, 154, 129 on videotaped encounters between individually-housed, male Swiss mice and anosmic male 'standard opponents' were assessed using a variety of ethological analyses. The effects of drugs were studied on individual elements and on the times allocated by subjects to broad categories of behaviour. Neither of the drugs significantly altered times allocated to broad categories of behaviour. Both doses of both compounds significantly increased the incidences of some 'fearful'/defensive postures. A more detailed analysis considered the effects of the drugs on the sequences of postures used in the resident's behaviour. This involved the generation of 'dendrograms' which provided support for the view that both naloxone and ICI 154, 129 altered the associations between behavioural elements seen in saline controls (especially at higher doses) and that the effects of these antagonists were qualitatively different.

Effects of intraventricular injection of delta receptor antagonist ICI 154, 129 on the secretion of luteinizing hormone and prolactin in the proestrous rat.[Pubmed:1661235]

Endocrinol Jpn. 1991 Apr;38(2):213-8.

In order to ascertain the role of delta receptors in the control of gonadotropin secretion, a preferential delta receptor antagonist ICI 143,129 was microinjected into the third ventricle through chronically implanted cannulae and the effects on the serum concentration of luteinizing hormone (LH) and prolactin (PRL) were determined in female rats in proestrus. When the injection was given at 1030 h, ICI 154,129 (50 micrograms) exerted no significant effects on either LH or PRL. However, in the rat given a microinjection of ICI 154,129 at 1300 h, an afternoon rise in LH occurred in advance and was of greater magnitude, with the peak time more than 1 h earlier and the peak amplitude approximately 100% greater than that in the control rat, respectively. The injection also suppressed the PRL rise during the plateau phase. The results indicate that delta receptors are involved in the mediation of the inhibitory influence of endogenous opioids on the surge of LH in proestrus, and that delta receptors mediate the facilitatory influence of opioids on the PRL surge during the plateau phase.

Comparison of the influence of the opiate delta receptor antagonist, ICI 154,129, and naloxone on social interaction and behaviour in an open field.[Pubmed:6325983]

Neuropharmacology. 1984 Jan;23(1):13-7.

The influence of a novel opiate delta receptor antagonist, ICI 154,129, and naloxone on social interaction and on behaviour in an open field were compared. At a dose thought to optimally block the delta receptor, ICI 154,129 produced open field behaviour typical of a non-emotional animal: this drug decreased social investigation and the latency to attack. In contrast, naloxone was largely without effect in these tests.

ICI 154,129, a delta-opioid receptor antagonist raises seizure threshold in rats.[Pubmed:6321207]

Eur J Pharmacol. 1984 Jan 13;97(1-2):141-4.

Acute i.c.v. administration of ICI 154,129 (100-600 micrograms), a delta-opioid receptor antagonist, raised the seizure threshold in a dose-related manner in rats exposed to flurothyl, a volatile convulsant. Pretreatment with naloxone or beta-funaltrexamine (beta-FNA) antagonized this effect. Lower doses of ICI 154,129 (12.5-50 micrograms), which did not influence seizure threshold, selectively antagonized the anticonvulsant action of [D-Ala2,D-Leu5]enkephalin (DADLE) in the same procedure. Consequently, it may be inferred that ICI 154,129 at high doses has mu-agonist and at low doses delta-antagonist properties in the rat flurothyl test.

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