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| Targets |
Unlike its parent compound Golgicide A, which targets the secretory pathway protein GBF1 (Golgi-specific Brefeldin A resistance factor 1), Golgicide A-1 is reported to be a less active cis-diastereomer. It weakly inhibits mosquito reproduction, but its primary utility is as a pharmacological tool to study off-target effects.
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| ln Vitro |
In the Aedes aegypti and Anopheles stephensi larvae experiment, glyphicide A-1 (GCA-1) exhibits negligible to no cytotoxicity[1].
In vitro, Golgicide A-1 displays minimal to no cytotoxicity in Aedes aegypti and Anopheles stephensi larvae assays. It serves as a negative control in experiments where Golgicide A is used to study GBF1 inhibition. The compound shows only weak activity compared to its trans-diastereomer counterpart. |
| ln Vivo |
In vivo, Golgicide A-1 weakly inhibits mosquito reproduction. Because it is significantly less active than Golgicide A, it is frequently used as a control in live-animal studies to confirm that observed biological effects (e.g., on insect development) are specifically due to GBF1 inhibition and not general toxicity from the chemical scaffold.
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| Enzyme Assay |
As a non-cellular control, Golgicide A-1 is used in in vitro biochemical assays to validate target engagement. It is added at concentrations similar to Golgicide A (e.g., 0.1-100 microM) to enzyme preparations or cell lysates, and the lack of inhibition of GBF1-dependent ARF1-GTP activation or Golgi disruption confirms the specificity of Golgicide A.
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| Cell Assay |
Standard cellular assays involve immunofluorescence microscopy of the Golgi apparatus. Cells (e.g., HeLa or BSC-1) are treated with Golgicide A-1 (5-50 uM) for 1-24 hours alongside Golgicide A. After fixation, cells are stained with a Golgi marker (e.g., GM130 antibody). Golgicide A-1 is expected to show minimal fragmentation or redistribution of the Golgi apparatus, confirming its use as an inactive control.
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| Animal Protocol |
Larval toxicity assays in mosquitoes are used for in vivo evaluation. Aedes aegypti or Anopheles stephensi larvae are placed in multiwell plates containing water. Golgicide A-1 is added at concentrations ranging from 1-100 uM, and mortality is recorded at 24 and 48 hours. Minimal to no mortality compared to the active Golgicide A confirms the lack of toxicity and validates the specificity of the active compound.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Golgicide A-1 is not well-documented. As a small molecule with molecular weight 284.31 (C17H14F2N2), it likely shares similar solubility characteristics with Golgicide A. It is soluble in DMSO (110 mg/mL) and is typically stored as a powder at -20degC. It is not intended for pharmaceutical development, so detailed PK studies are rarely performed.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Golgicide A-1 indicates minimal to no cytotoxicity at effective concentrations used in mosquito assays. It is generally regarded as safe for laboratory use as a research control. However, as an experimental chemical, standard safety precautions should be taken. It is not intended for human therapeutic use and has no clinical safety profile.
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| References |
[1]. Daniel J Mack, et al. Distinct biological effects of golgicide a derivatives on larval and adult mosquitoes. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5177-81.
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| Additional Infomation |
(3aR,4S,9bS)-golgicide A is a 6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopentano[c]quinoline with the 3aR,4S,9bS configuration. It is the enantiomer of (3aS,4R,9bR)-golgicide A.
Golgicide A-1 is the cis-diastereomer of Golgicide A, specifically characterized by a cis configuration of the fused cyclopenta[c]quinoline ring system. Its chemical name is 3-[(3aR,4S,9bS)-6,8-difluoro-3H,3aH,4H,5H,9bH-cyclopenta[c]quinolin-4-yl]pyridine. It is an important chemical control for distinguishing specific GBF1-mediated effects from non-specific cytotoxicity in Golgi-related research. |
| Molecular Formula |
C17H14F2N2
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|---|---|
| Molecular Weight |
284.30
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| Exact Mass |
284.112
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| CAS # |
1394285-49-4
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| Related CAS # |
Golgicide A;1139889-93-2;Golgicide A-2;1394285-50-7;(Rac)-Golgicide A;1005036-73-6
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| PubChem CID |
1085377
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| Appearance |
White to light yellow solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
414
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C=C[C@H]2[C@@H]1[C@H](NC3=C2C=C(C=C3F)F)C4=CN=CC=C4
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| InChi Key |
NJZHEQOUHLZCOX-WOSRLPQWSA-N
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| InChi Code |
InChI=1S/C17H14F2N2/c18-11-7-14-12-4-1-5-13(12)16(10-3-2-6-20-9-10)21-17(14)15(19)8-11/h1-4,6-9,12-13,16,21H,5H2/t12-,13+,16+/m0/s1
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| Chemical Name |
(3aR,4S,9bS)-6,8-difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
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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: 110 mg/mL (386.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5.5 mg/mL (19.35 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 55.0 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: ≥ 5.5 mg/mL (19.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 55.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5174 mL | 17.5871 mL | 35.1741 mL | |
| 5 mM | 0.7035 mL | 3.5174 mL | 7.0348 mL | |
| 10 mM | 0.3517 mL | 1.7587 mL | 3.5174 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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