VUF 8430 dihydrobromidePotent, high affinity H4 agonist CAS# 100130-32-3 |
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Quality Control & MSDS
3D structure
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| Cas No. | 100130-32-3 | SDF | Download SDF |
| PubChem ID | 3063227 | Appearance | Powder |
| Formula | C4H13Br2N5S | M.Wt | 323.05 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water and to 100 mM in DMSO | ||
| Chemical Name | 2-(diaminomethylideneamino)ethyl carbamimidothioate;dihydrobromide | ||
| SMILES | C(CSC(=N)N)N=C(N)N.Br.Br | ||
| Standard InChIKey | GPWJSTKHQMIXCA-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C4H11N5S.2BrH/c5-3(6)9-1-2-10-4(7)8;;/h1-2H2,(H3,7,8)(H4,5,6,9);2*1H | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | High affinity (pKi = 7.5), potent histamine H4 receptor full agonist (pEC50 = 7.3). Displays moderate affinity for H3 receptors (pKi = 6.0) and weak partial agonist activity at H2 receptors. |
VUF 8430 dihydrobromide Dilution Calculator
VUF 8430 dihydrobromide Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0955 mL | 15.4775 mL | 30.955 mL | 61.9099 mL | 77.3874 mL |
| 5 mM | 0.6191 mL | 3.0955 mL | 6.191 mL | 12.382 mL | 15.4775 mL |
| 10 mM | 0.3095 mL | 1.5477 mL | 3.0955 mL | 6.191 mL | 7.7387 mL |
| 50 mM | 0.0619 mL | 0.3095 mL | 0.6191 mL | 1.2382 mL | 1.5477 mL |
| 100 mM | 0.031 mL | 0.1548 mL | 0.3095 mL | 0.6191 mL | 0.7739 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors.[Pubmed:18635748]
J Pharmacol Exp Ther. 2008 Oct;327(1):88-96.
Using the natural variation in histamine H(4) receptor protein sequence, we tried to identify amino acids involved in the binding of H(4) receptor agonists. To this end, we constructed a variety of chimeric human-mouse H(4) receptor proteins to localize the domain responsible for the observed pharmacological differences between human and mouse H(4) receptors in the binding of H(4) receptor agonists, such as histamine, clozapine, and VUF 8430 [S-(2-guanidylethyl)-isothiourea]. After identification of a domain between the top of transmembrane domain 4 and the top of transmembrane domain 5 as being responsible for the differences in agonist affinity between human and mouse H(4)Rs, detailed site-directed mutagenesis studies were performed. These studies identified Phe(169) in the second extracellular loop as the single amino acid responsible for the differences in agonist affinity between the human and mouse H(4)Rs. Phe(169) is part of a Phe-Phe motif, which is also present in the recently crystallized beta(2)-adrenergic receptor. These results point to an important role of the second extracellular loop in the agonist binding to the H(4) receptor and provide a molecular explanation for the species difference between human and mouse H(4) receptors.
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.[Pubmed:17154494]
J Med Chem. 2006 Nov 16;49(23):6650-1.
During an in-house database screen, we identified S-(2-guanidylethyl)-isothiourea as a high affinity agonist for the histamine H4 receptor, with a 33-fold selectivity over the histamine H3 receptor and negligible affinity for the other histamine receptor subtypes. This nonimidazole ligand is introduced as a useful and complementary pharmacological tool that enables further unraveling of the physiological roles of the H4 receptor.
The influence of guanidino and isothiourea groups in histaminergic compounds on H2-activity.[Pubmed:2942013]
Agents Actions. 1986 Apr;18(1-2):137-40.
Because in some alkylenediisothioureas replacement of one of the isothiourea groups by a guanidino group resulted in a strong increase in agonistic histamine H2-activity, while replacement of the guanidino group of a potent analogue of impromidine by an isothiourea group resulted in a complete loss of histamine H2-activity, it was concluded that guanidino and isothiourea groups are not bio-isosteric for the H2-receptor.
