| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Emodepside (also known as BAY 44-4400 and PF 1022-221) is a novel and potent cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside is effective against a number of gastrointestinal nematodes, and is approved for use in cats. It belongs to the class of drugs known as the octadepsipeptides, a relatively new class of anthelmintic (research into these compounds began in the early 1990s), which are suspected to achieve their anti-parasitic effect by a novel mechanism of action due to their ability to kill nematodes resistant to other anthelmintics.
| ln Vitro |
The semisynthetic derivative emodepside of PF1022A has a para-positional morpholine attached to each of the two D-phenyllactic acids. Emodepside works well against a range of nematodes that invade the gastrointestinal tract. In nematodes, emodepside binds to a presynaptic latrophilin receptor[1]. Emodepside causes a slow, concentration-dependent, time-dependent (20 min) hyperpolarization and increase in voltage-activated K currents. It is also sensitive to 4-aminopyridine.Emodepside inhibits the process of spiking. The ryanodine spike frequency increase between 20 and 35 minutes is significantly inhibited by emodepside, with a reduction of 9.8 spikes/min[2]. When emodepside is present, significantly elevated currents are detected without depolarization up to a 0 mV threshold and without the need for extra stimuli to fictitiously raise [Ca 2+]i levels. These new discoveries verify that emodepside directly targets Slo-1[3].
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| ln Vivo |
Emodepside inhibits three crucial physiological processes: feeding, reproduction, and locomotion. It does this by interfering with signaling at the neuromuscular junction on the pharynx, body-wall muscles, and egg-laying muscles[4].
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| References |
| Molecular Formula |
C60H90N6O14
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|---|---|
| Molecular Weight |
1119.3884
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| Exact Mass |
1,118.65
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| Elemental Analysis |
C, 64.38; H, 8.10; N, 7.51; O, 20.01
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| CAS # |
155030-63-0
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| Related CAS # |
1610546-58-1 (with toltrazuril);155030-63-0;
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| Appearance |
Solid powder
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| SMILES |
O=C([C@H](CC(C)C)N(C)C([C@@H](C)OC([C@H](CC(C)C)N(C)C([C@@H](CC1=CC=C(N2CCOCC2)C=C1)OC([C@H](CC(C)C)N(C)C([C@@H](C)OC([C@H](CC(C)C)N3C)=O)=O)=O)=O)=O)=O)O[C@H](CC4=CC=C(N5CCOCC5)C=C4)C3=O
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| InChi Key |
ZMQMTKVVAMWKNY-YSXLEBCMSA-N
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| InChi Code |
InChI=1S/C60H90N6O14/c1-37(2)31-47-57(71)77-41(9)53(67)61(11)50(34-40(7)8)60(74)80-52(36-44-17-21-46(22-18-44)66-25-29-76-30-26-66)56(70)64(14)48(32-38(3)4)58(72)78-42(10)54(68)62(12)49(33-39(5)6)59(73)79-51(55(69)63(47)13)35-43-15-19-45(20-16-43)65-23-27-75-28-24-65/h15-22,37-42,47-52H,23-36H2,1-14H3/t41-,42-,47+,48+,49+,50+,51-,52-/m1/s1
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| Chemical Name |
(3S,6R,9S,12R,15S,18R,21S,24R)-3,9,15,21-tetraisobutyl-4,6,10,16,18,22-hexamethyl-12,24-bis(4-morpholinobenzyl)-1,7,13,19-tetraoxa-4,10,16,22-tetraazacyclotetracosan-2,5,8,11,14,17,20,23-octaone
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| Synonyms |
PF 1022-221; PF-1022 221; PF-1022-221; BAY 444400; BAY444400; BAY-444400; BAY 44-4400; BAY44-4400; BAY-44-4400;
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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 |
| 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 : 100~120 mg/mL ( 89.33~107.20 mM )
Ethanol : ~20 mg/mL H2O :< 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 3 mg/mL (2.68 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 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: 3 mg/mL (2.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 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: ≥ 3 mg/mL (2.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3 mg/mL (2.68 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8933 mL | 4.4667 mL | 8.9334 mL | |
| 5 mM | 0.1787 mL | 0.8933 mL | 1.7867 mL | |
| 10 mM | 0.0893 mL | 0.4467 mL | 0.8933 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.
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