| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Bromocriptine Mesylate (CB154) is a dopamine D2/3 agonist (with pKi of 8.05±0.2 for D2) for the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.
| Targets |
D2 receptor( Ki = 12.2 nM ); D3 receptor ( Ki = 12.2 nM ); D4 receptor ( Ki = 59.7 nM ); D1 receptor ( Ki = 1659 nM ); D5 receptor ( Ki = 1691 nM )
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| ln Vitro |
Bromocriptine stimulates [35S]-GTPγS binding at the 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. Bromocriptine (BKT), an ergot alkaloid, is found to be weakly active against inducible macrophage NOS (IC50>100 μM), but it acts as a strong inhibitor of purified neuronal nitric oxide synthase (NOS) (IC50=10±2 μM) [2]. It has been discovered that at least one human cytochrome P450 enzyme is inhibited by bromocriptine. With an estimated IC50 value for the interaction of 1.69 μM, bromocriptine is a strong inhibitor of CYP3A4[3].
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| ln Vivo |
Bromocriptine mesylate (2 mg/kg, i.p.) is given for 7 days in groups of mice participating in the forced swimming test (FST) and tail suspension test (TST). Bromocriptine group exhibits a discernible anti-immobility effect in comparison to the control. The anti-immobility effect of MPE (200 mg/kg, p.o.) is significantly and dose-dependently potentiated when bromocriptine is given 30 minutes after the final dose of the seven-day MPE treatment and the subjects are exposed to FST, in contrast to MPE treatment alone. When compared to the control group, the group receiving bromocriptine treatment exhibits a notable decrease in immobility time. When bromocriptine (100 and 200 mg/kg, p.o.) is administered seven days after MPE pretreatment, the anti-immobility effect of MPE is significantly and dose-dependently enhanced, as compared to MPE treatment alone[4]. When bromocriptine is administered intraceremoniously, the static mechanical allodynia (SMA) score is significantly lower than in sham (saline-injected rats) and the effect lasts for 30 minutes. In the CCI-IoN group, intraperitoneal administration of bromocriptine resulted in a significant, dose-dependent (0.1 mg and 1 mg/kg) decrease in pain scores compared to sham, with a 6-hour duration of effect. The biggest reduction in score is induced by the highest dose (P<0.01). For 20 minutes, bromocriptine has an effect. When compared to a sham group, the CCI-IoN+6-OHDA lesioned group's SMA score significantly decreases upon intraperitoneal administration of bromocriptine. Its impact lasts for half an hour[5].
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| Enzyme Assay |
The assay for [35S]-GTPγS binding is performed. For 30 minutes at 30°C, cell membranes (25 ±75 ug) are incubated in Buffer B, which contains 0.1 mM dithiothreitol (DTT), 1 uM GDP, and medications in a volume of 0.9 mL. This preincubation guarantees that the tested agonists are in an equilibrium state when the final concentration of [35S]-GTPγS (50±150 pM) is added (in 100 uL of Buffer B) to start the reaction. Unless otherwise specified, the assay mixture is incubated for a further 20 minutes. Rapid filtration ends the assays, and bound radioactivity is measured as previously mentioned for the radio-ligand binding assays. Less than 20% of the added GTPγS is bound in total by [35S]-GTPγS[1].
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| Animal Protocol |
Mice: There are 150 total Swiss mice (20–25 g) of either sex used. One such agonist for the dopamine receptor (D2) is bromocriptine mesylate. Distilled water is used to dilute the medication haloperidol, which is then injected. A single drop of glacial acetic acid is used to dissolve bromocriptine mesylate, which is then diluted with distilled water to the desired volume. Imipramine dissolves in 0.9% regular saline. In groups of mice undergoing the Forced Swimming Test (FST) and Tail Suspension Test (TST), haloperidol (0.1 mg/kg, i.p.) and bromocriptine mesylate (2 mg/kg, i.p.) are given for 7 days. As a standard, positive control groups receive imipramine (10 mg/kg, p.o.) for seven days.
Rats: The rats used are adult male Sprague-Dawleys (N=112, 275–325 g). A couple of weeks following the 6-OHDA injection, the animals undergo a brief (less than three minutes) mask-applied 2% halothane anesthesia before receiving either the vehicle (5 μL of 0.9% saline) or bromocriptine (7 μg/kg dissolved in 5 μL vehicle) intraperitoneally. We used concentrations of SKF81297 (3 mg/kg dissolved in 0.9% saline) and bromocriptine (1 mg/kg) for intraperitoneal injection. A blind experimenter places the rats in the observation field for a 40-minute period test after they have recovered for less than two minutes. |
| References |
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| Molecular Formula |
C33H44BRN5O8S
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|---|---|
| Molecular Weight |
750.700160000001
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| Exact Mass |
749.21
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| Elemental Analysis |
C, 52.80; H, 5.91; Br, 10.64; N, 9.33; O, 17.05; S, 4.27
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| CAS # |
22260-51-1
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| Related CAS # |
Bromocriptine; 25614-03-3
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| Appearance |
Solid powder
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| SMILES |
CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]3(N1C(=O)[C@](O3)(C(C)C)NC(=O)[C@H]4CN([C@@H]5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O.CS(=O)(=O)O
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| InChi Key |
NOJMTMIRQRDZMT-GSPXQYRGSA-N
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| InChi Code |
InChI=1S/C32H40BrN5O5.CH4O3S/c1-16(2)12-24-29(40)37-11-7-10-25(37)32(42)38(24)30(41)31(43-32,17(3)4)35-28(39)18-13-20-19-8-6-9-22-26(19)21(27(33)34-22)14-23(20)36(5)15-18;1-5(2,3)4/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39);1H3,(H,2,3,4)/t18-,23-,24+,25+,31-,32+;/m1./s1
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| Chemical Name |
(6aR,9R)-5-bromo-N-[(1S,2S,4R,7S)-2-hydroxy-7-(2-methylpropyl)-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide;methanesulfonic acid
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| Synonyms |
CB154; CB-154; CB 154; Bromocriptine Mesylate; 2-Bromoergocryptine Mesylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100~250 mg/mL (133.2~333.0 mM)
H2O: ~1.1 mg/mL (~1.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04128683 | Active Recruiting |
Drug: amisulpride Drug: bromocriptine |
Anorexia Nervosa | University of California, San Diego |
October 20, 2020 | Early Phase 1 |
| NCT03575000 | Not yet recruiting | Drug: Bromocriptine | Schizophrenia Glucose Intolerance |
VA Pittsburgh Healthcare System | November 1, 2023 | Phase 4 |
| NCT05180773 | Recruiting | Drug: Bromocriptine Drug: Placebo Drug: Rivaroxaban Drug: Second Placebo |
Peripartum Cardiomyopathy, Postpartum |
Dennis M. McNamara, MD, MS | July 27, 2022 | Phase 4 |
| NCT02428946 | Completed | Drug: Bromocriptine | Insulin Sensitivity | Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) |
October 2014 | Not Applicable |
| NCT02544321 | Completed | Drug: Bromocriptine Other: Placebo |
Type 1 Diabetes | University of Colorado, Denver | September 2015 | Phase 2 |
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