受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H27ClN2O.2HCl |
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分子量 | 479.87 | CAS No. | 193611-72-2 | ||||
Solubility (25°C)* | 体外 | DMSO | 96 mg/mL (200.05 mM) | ||||
Ethanol | 40 mg/mL (83.35 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. |
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in vitro | BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 µM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. [1] In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). [2] The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. [3] The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. [4] |
in vivo | In diabetic pithed rats, administration of the selective 5-HT1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694,247 (50 μg/kg), a selective agonist for non-rodent 5-HT1B and 5-HT1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572. [5] |
特徴 | A selective 5-HT1D/1B receptor antagonist. |
細胞アッセイ | 細胞株 | CHO cells expressing the h5-HT1B or h5-HT1D receptors |
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濃度 | 0 μM -10 μM | |
反応時間 | 30 minutes | |
実験の流れ | [35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106 cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 µ M), with or without BRL-15572. The reaction is started by the addition of 10 µL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Non-specific binding is determined by addition of unlabelled GTPγS (10 µM), prior to the addition of cells. The reaction is stopped by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Radioactivity is determined by liquid scintillation spectrometry. | |
動物実験 | 動物モデル | Male Wistar rats with diabetes |
投薬量 | 1 mg/kg, 2 mg/kg | |
投与方法 | Administered via i.v. |
VEGFR2 promotes central endothelial activation and the spread of pain in inflammatory arthritis [Beazley-Long N Brain Behav Immun, 2018, 74:49-67] | PubMed: 29548992 |
An In Vitro Model for Identifying Cardiac Side Effects of Anesthetics [Chang ACY Anesth Analg, 2018, 10.1213/ANE.0000000000003757] | PubMed: 30198930 |
Methamphetamine modulates the production of interleukin-6 and tumor necrosis factor-alpha via the cAMP/PKA/CREB signaling pathway in lipopolysaccharide-activated microglia [Wang B Int Immunopharmacol, 2018, 56:168-178] | PubMed: 29414647 |
The role of PDE3B phosphorylation in the inhibition of lipolysis by insulin [DiPilato LM Mol Cell Biol, 2015, 35(16):2752-60] | PubMed: 26031333 |
Rapamycin prevents strong phosphorylation of p53 on serine 46 and attenuates activation of the p53 pathway in A549 lung cancer cells exposed to actinomycin D [Krześniak M Mech Ageing Dev, 2014, 139:11-21] | PubMed: 24915467 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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