1. GPCR/G Protein
    Neuronal Signaling
    Autophagy
  2. Dopamine Receptor
    Autophagy
  3. Bromocriptine mesylate

Bromocriptine mesylate (Synonyms: CB-154)

製品番号: HY-12705A 純度: 99.98%
取扱説明書

Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.

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Bromocriptine mesylate 構造式

Bromocriptine mesylate 構造式

CAS 番号 : 22260-51-1

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 66 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 78 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.

IC50 & Target

pKi: 8.05±0.2 (dopamine D2 receptor)[1]

体外実験

Bromocriptine stimulates [35S]-GTPγS binding at D2 dopamine receptor expressed in CHO cells with pEC50 of 8.15±0.05[1]. Bromocriptine also is a strong inhibitor of brain nitric oxide synthase. The ergot alkaloid Bromocriptine (BKT) is found to act as a strong inhibitor of purified neuronal nitric oxide synthase (NOS) (IC50=10±2 μM) whereas it is poorly active towards inducible macrophage NOS (IC50>100 μM) [2]. Bromocriptine is found to inhibit the activity of at least one human cytochrome P450 enzyme. Bromocriptine is a potent inhibitor of CYP3A4 with a calculated IC50 value for the interaction of 1.69 μM[3].

体内実験

Bromocriptine mesylate (2 mg/kg, i.p.) is administered for 7 days in groups of mice in forced swimming test (FST) and tail suspension test (TST). Bromocriptine group shows significant anti-immobility action as compared to control. When Bromocriptine administered 30 min after the last dose of 7 days MPE treatment and subjected to FST, this dopaminergic agonist produces significant and dose dependent potentiation of anti-immobility action of MPE (200 mg/kg, p.o.) as compared to MPE treatment alone. Bromocriptine treatment group shows a significant reduction of immobility time as compared to control. Bromocriptine administration after 7 days pretreatment with MPE (100 and 200 mg/kg, p.o.) shows significant and dose dependent potentiation of anti-immobility action of MPE as compared to MPE treatment alone[4]. Intracisternal administration of Bromocriptine decreases significantly the static mechanical allodynia (SMA) score compared to that of sham (saline-injected rats) and its effect lasted for 30 min. Intraperitoneal administration of Bromocriptine induces a significant, dose dependent (0.1 mg and 1 mg/kg) decrease in pain scores in CCI-IoN group when compared to sham and its effect lasted for 6 h. The highest dose induces the highest score decrease (P<0.01). Bromocriptine effect lasts for 20 min. Intraperitoneal administration of Bromocriptine induces a significant dose dependent decrease in SMA score in CCI-IoN+6-OHDA lesioned group compared to that of sham. Its effect lasts for 6 h[5].

臨床実験
分子量

750.70

分子式

C₃₃H₄₄BrN₅O₈S

CAS 番号

22260-51-1

SMILES

[H][[email protected]@]12CC3=C(Br)NC4=CC=CC(C1=C[[email protected]@H](C(N[[email protected]@]5(C(C)C)C(N6[[email protected]@H](CC(C)C)C(N7CCC[[email protected]]7([[email protected]]6(O)O5)[H])=O)=O)=O)CN2C)=C43.OS(=O)(C)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度
体外: 

DMSO : 75 mg/mL (99.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3321 mL 6.6605 mL 13.3209 mL
5 mM 0.2664 mL 1.3321 mL 2.6642 mL
10 mM 0.1332 mL 0.6660 mL 1.3321 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (3.33 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.33 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
キナーゼ実験
[1]

The [35S]-GTPγS binding assay is carried out. Cell membranes (25 ±75 ug) are incubated in Buffer B containing 0.1 mM dithiothreitol (DTT) and 1 uM GDP and drugs in a volume of 0.9 mL for 30 min at 30°C. This preincubation ensures that the agonists tested are at equilibrium when the [35S]-GTPγS (50±150 pM, final concentration) is added (in 100 uL of Buffer B) to initiate the reaction. The assay mixture is incubated for a further 20 min unless otherwise stated. The assays are terminated by rapid filtration and bound radio-activity determined as described for the radio-ligand binding assays above. The total binding of [35S]-GTPγS is less than 20% of that added[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[4][5]

Mice[4]
Swiss mice (20-25 g) of either sex (total 150) are used. Bromocriptine mesylate is used as dopamine receptor (D2) agonist. Haloperidol is diluted in distilled water which is used for a vehicle of injection. Bromocriptine mesylate is dissolved in one drop of glacial acetic acid and made up to volume in distilled water. Imipramine is dissolved in 0.9% normal saline. Haloperidol (0.1 mg/kg, i.p.) and Bromocriptine mesylate (2 mg/kg, i.p.) are administered for 7 days in groups of mice in Forced Swimming Test (FST) and Tail Suspension Test (TST). Imipramine (10 mg/kg, p.o.) as a standard is administered in positive control groups for 7 days.
Rats[5]
Adult male Sprague-Dawley rats (N=112, 275-325 g) are used. Two weeks after the 6-OHDA injection, the animals are briefly (<3 min) anesthetized with 2 % halothane using a mask and received for intracisternal administration Bromocriptine (7 μg/kg dissolved in 5 μL vehicle) or the vehicle alone (5 μL of 0.9 % saline). For i.p. injection we used Bromocriptine (1 mg/kg) and SKF81297 (3 mg/kg dissolved in 0.9 % saline) concentrations. Following a recovery period (<2 min), the rats are placed in the observation field for 40 min period-test by a blind-experimenter.

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 99.98%

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Keywords:

BromocriptineCB-154CB154CB 154Dopamine ReceptorAutophagyInhibitorinhibitorinhibit

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製品名:
Bromocriptine mesylate
製品番号:
HY-12705A
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