Ivermectin B1a (Synonyms: dihydro Avermectin B1a,22,23-dihydro Avermectin B1a) |
| Catalog No.GC12700 |
Avermectin B1a의 유도체인 Ivermectin B1a는 Ivermectin의 주성분입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 71827-03-7
Sample solution is provided at 25 µL, 10mM.
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Ivermectin B1a is the main component (not less than 80%) of the anthelmintic, ivermectin. Ivermectin is one of the most useful veterinary antiparasitic drugs ever produced. Ivermectin belongs to the macrocyclic lactone class of avermectins. Ivermectin contains two homologous compounds, H2B1a and H2B1b. Avermectins are potent insecticidal, anthelmintic and acaricidal compounds in mediating the paralysis of nematodes and certain classes of ectoparasites by increasing the membrane permeability to chlorine ions[1].
In humans, ivermectin has been used to treat African river blindness (onchocerciasis). Ivermectin significantly decreased the prevalence of skin and eye diseases linked to this infection [2]. Ivermectin B1a produced antiparasitic activity via an interaction with a common receptor molecule, glutamate-gated chloride channels, which virtually expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function. The EC50 of ivermectin was 104 nM [1,3].
References:
[1] J. Wolsetnholme and A. T. Rogers. Glutamate-gated chloride channels and the mode of action of the avermectin/milbemycin anthelmintics. Parasitology131 Suppl, S85-S95 (2005).
[2] S. Gaisser, L. Kellenberger, A. L. Kaja, et al. Direct production of ivermectin-like drugs after domain exchange in the avermectin polyketide synthase of Streptomyces avermitilis ATCC31272. Organic & Biomolecular Chemistry 1(16), 2840-2847 (2003).
[3] J. P. Arena, K. K. Liu, P. S. Paress, et al. The mechanism of action of avermectins in Caenorhabditis elegans: Correlation between activation of glutamate-sensitive chloride current, membrane binding, and biological activity. Journal of Parasitology 81, 286-294 (1995).
| Cas No. | 71827-03-7 | SDF | |
| Synonyms | dihydro Avermectin B1a,22,23-dihydro Avermectin B1a | ||
| Chemical Name | 5-O-demethyl-22,23-dihydro-avermectin A1a | ||
| Canonical SMILES | C/C([C@@H](O[C@@]1([H])C[C@H](OC)[C@@H](O[C@]2([H])O[C@@H](C)[C@H](O)[C@@H](OC)C2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@]4([H])C5=O)=C\C[C@]6([H])C[C@@](O5)([H])C[C@]7(CC[C@H](C)[C@]([C@H](CC)C)([H])O7)O6 | ||
| Formula | C48H74O14 | M.Wt | 875.1 |
| Solubility | DMSO : 100 mg/mL (114.27 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.1427 mL | 5.7136 mL | 11.4273 mL |
| 5 mM | 0.2285 mL | 1.1427 mL | 2.2855 mL |
| 10 mM | 0.1143 mL | 0.5714 mL | 1.1427 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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