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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Halofenozide targets the ecdysone receptor, a nuclear hormone receptor in insects. By binding to ecdysone receptors, it disrupts molting and pupation, leading to premature death of targeted pests. It acts as an ecdysteroid agonist, mimicking the biological function of 20-hydroxyecdysone and causing premature molting. Due to its selective action on insect endocrine systems, halofenozide has minimal effects on mammals.
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| ln Vitro |
In vitro oocyte growth and development are inhibited by halofenozide (RH-0345) [1].
In vitro, halofenozide demonstrates agonist activity at the ecdysone receptor. Its activity is typically assessed using reporter gene assays, with an EC₅₀ of 457 nM for agonist activity at the ecdysone receptor in Spodoptera littoralis Sl2 cells. The compound's insecticidal activity has been evaluated at different concentrations ranging between 8 and 32 micrograms/L. |
| ln Vivo |
Following the topical administration of halobenzohydrazide (RH-0345; 5 and 10 μg) to mature females, the maximum dosage (10 μg) notably decreased scores for three reproductive parameters: fecundity, egg viability, and oviposition period [1]. Eggs exposed to halofenyl hydrazide at two tested concentrations (5 and 10 μg) showed reduced length, breadth, and volume [1].
In vivo, halofenozide induces a precocious and incomplete molt in several insect orders. It affects the corpora allata and reproductive physiology of insects, such as the Formosan subterranean termite. The compound causes premature molting and interferes with normal growth and development in insects. Its effects on ecdysteroid titers have been measured using enzyme immunoassays. Halofenozide has been studied for its effects on reproduction in mealworm (Tenebrio molitor). |
| Enzyme Assay |
Cell-free receptor binding assays for halofenozide involve assessing its affinity for the ecdysone receptor. The binding affinity can be determined using competition binding assays with radiolabeled ecdysone or by using a Lineweaver-Burk assay. These assays measure the ability of halofenozide to displace the natural ligand from the receptor, providing information on its binding affinity and mechanism of action as an ecdysteroid agonist.
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| Cell Assay |
Cell viability assay [2]
Cell Types: ovaries dissected and cultured from adult female mealworms, T. molitor Tested Concentrations: 1 μM and 10 μM Incubation Duration: 4 days Experimental Results: No significant effect on the amount of ecdysteroids The effects were in culture medium using 0-day-old and 2-day-old female ovaries at a concentration of 10 μM. A concentration of 1 μM in culture medium and 2-day-old ovaries caused a small significant increase in ovarian ecdysteroid content in the culture medium. In vitro cellular assays for halofenozide typically use insect cell lines expressing the ecdysone receptor. Spodoptera littoralis Sl2 cells are treated with halofenozide at various concentrations, and ecdysone receptor activation is measured using a luciferase reporter gene assay. The EC₅₀ is calculated from the dose-response curve. These assays confirm the compound's agonist activity and potency at the receptor level. |
| Animal Protocol |
Animal/Disease Models: Emerging (0 days old) adult female yellow stork [1]
Doses: 5 and 10 μg Route of Administration: Topical application Experimental Results: Resulted in smaller eggs in length, width and volume at both test doses diminished (5 and 10 μg). In vivo animal studies for halofenozide are conducted in insect models. The insecticidal activity is evaluated by exposing insects to various concentrations of halofenozide and monitoring mortality, molting abnormalities, and developmental effects. Studies have assessed the significance of absorption, oxidation, and binding to toxicity in multi-resistant cotton leafworm. The compound's effects on ecdysteroid production and protein analysis have been studied in mealworm pupae. |
| ADME/Pharmacokinetics |
Halofenozide has a molecular formula of C₁₈H₁₉ClN₂O₂ and a molecular weight of 330.81. It is stable as a powder under standard storage conditions. The compound is a dibenzoylhydrazine-based nonsteroidal insecticide. Due to its selective action on insect endocrine systems, it has minimal effects on mammals. It is for research use only and is not for therapeutic use.
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| Toxicity/Toxicokinetics |
Non-Human Toxicity Values
Rat inhalation LC50 >2.7 mg/L/4 hours; Rabbit dermal LD50 >2000 mg/kg; Mouse oral LD50 2214 mg/kg; Rat oral LD50 2850 mg/kg |
| References |
[1]. Faïza Taïbi, et al. Effect of ecdysone agonist RH-0345 on reproduction of mealworm, Tenebrio molitor. Comp Biochem Physiol C Toxicol Pharmacol. 2003 Jul;135C(3):257-67.
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| Additional Infomation |
Artenin is a dihydrazide insecticide belonging to the monochlorobenzene class of compounds. Its function is similar to that of N'-benzoyl-N-(tert-butyl)benzoin. Mechanism of action: Ecdyskinin agonist, causing premature molting in insects; insect growth regulator.
Halofenozide is also known as RH-0345. It belongs to a new group of insect growth regulators (IGRs) with a benzoylhydrazine structure. The compound is particularly effective against lepidopteran larvae and certain turf-damaging insects. It is used as a tool in entomological research. Halofenozide is available as a commercial formulation (23% EC) for research purposes. |
| Molecular Formula |
C18H19CLN2O2
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| Molecular Weight |
330.81
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| Exact Mass |
330.114
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| CAS # |
112226-61-6
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| PubChem CID |
114994
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| Appearance |
White solid
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| Density |
1.205g/cm3
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| Melting Point |
198.0-199.0°
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| Index of Refraction |
1.584
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| LogP |
4.316
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(C)N(C(=O)C1=CC=CC=C1)NC(=O)C2=CC=C(C=C2)Cl
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| InChi Key |
CNKHSLKYRMDDNQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19ClN2O2/c1-18(2,3)21(17(23)14-7-5-4-6-8-14)20-16(22)13-9-11-15(19)12-10-13/h4-12H,1-3H3,(H,20,22)
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| Chemical Name |
N'-benzoyl-N'-tert-butyl-4-chlorobenzohydrazide
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| Synonyms |
RH-0345; RH 0345; Halofenozide
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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 : ~125 mg/mL (~377.86 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0229 mL | 15.1144 mL | 30.2288 mL | |
| 5 mM | 0.6046 mL | 3.0229 mL | 6.0458 mL | |
| 10 mM | 0.3023 mL | 1.5114 mL | 3.0229 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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