GR 94800

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Cat.No. 1667 - GR 94800 | N-(Bz)Ala-Ala-D-Trp-Phe-D-Pro-Pro-Nle-NH2 | CAS No. 141636-65-9
Description: Potent, selective NK2 antagonist
Datasheet
Citations

Biological Activity

Potent and selective tachykinin NK2 receptor antagonist (pKB values are 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors respectively). Active in vivo.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M. Wt 904.08
Formula C49H61N9O8
Sequence AAWFPPX

(Modifications: Ala-1 = N-(Bz)Ala, Trp-3 = D-Trp, Pro-5 = D-Pro, X = Nle with C-terminal amide)

Storage Desiccate at -20°C
CAS Number 141636-65-9
PubChem ID 5487475
InChI Key CWEISCOCKRHHOU-UJYVDGJVSA-N
Smiles [H]N([C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N1CCC[C@@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(N)=O)C(=O)C1=CC=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 4 mg/ml in ethanol

Preparing Stock Solutions

The following data is based on the product molecular weight 904.08. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.11 mL 5.53 mL 11.06 mL
5 mM 0.22 mL 1.11 mL 2.21 mL
10 mM 0.11 mL 0.55 mL 1.11 mL
50 mM 0.02 mL 0.11 mL 0.22 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Matuszek et al (1998) An investigation of tachykinin NK2 receptor subtypes in the rat. Eur.J.Pharmacol. 352 103 PMID: 9718274

McElroy et al (1992) Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J.Med.Chem. 35 2582 PMID: 1321907

Zagorodnyuk et al (1995) Evidence that tachykinin NK1 and NK2 receptors mediate non-adrenergic non-cholinergic excitation and contraction in the circular muscle of guinea-pig duodenum. Br.J.Pharmacol. 115 237 PMID: 7545517


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Keywords: Potent selective NK2 antagonists Tachykinin Receptors Neurokinin GR94800 GlaxoSmithKline GSK NK2 Receptor Peptide

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