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MedKoo Cat#: 513693 | Name: CID16020046
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CID16020046 is a selective GPR55 inverse agonist. CID16020046 is a G protein-coupled receptor that is weakly activated by some cannabinoids at nM concentrations. CID16020046 has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.

Chemical Structure

CID16020046
CID16020046
CAS#834903-43-4

Theoretical Analysis

MedKoo Cat#: 513693

Name: CID16020046

CAS#: 834903-43-4

Chemical Formula: C25H19N3O4

Exact Mass: 425.1376

Molecular Weight: 425.44

Elemental Analysis: C, 70.58; H, 4.50; N, 9.88; O, 15.04

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,150.00 2 Weeks
500mg USD 2,050.00 2 Weeks
1g USD 3,250.00 2 Weeks
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Related CAS #
No Data
Synonym
CID16020046; CID-16020046; CID 16020046.
IUPAC/Chemical Name
4-[4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxo-1,4-dihydropyrrolo[3,4-d]pyrazol-5-yl]benzoic acid
InChi Key
VGUQVYZXABOXCX-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H19N3O4/c1-14-5-7-15(8-6-14)21-20-22(27-26-21)24(30)28(18-11-9-16(10-12-18)25(31)32)23(20)17-3-2-4-19(29)13-17/h2-13,23,29H,1H3,(H,26,27)(H,31,32)
SMILES Code
O=C(O)C1=CC=C(N(C2=O)C(C3=CC=CC(O)=C3)C4=C2NN=C4C5=CC=C(C)C=C5)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot# C9M05C28
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM.
In vitro activity:
This study showed that AGEs dose dependently induced GPR55 expression in ATDC5 chondrocytes. The blockage of GPR55 by its newly discovered antagonist-CID16020046 mitigated AGEs- induced increase in cellular ROS and decrease in antioxidant NRF2. Reference: Chem Biol Interact. 2020 Jul 1;325:109088. https://pubmed.ncbi.nlm.nih.gov/32360554/
In vivo activity:
Further analysis of the component pain-related behaviours revealed that CID16020046 significantly reduced the duration of biting/licking/flinching behaviour (Pain 2) during the second phase of the formalin trial (Fig. 2C). Duration of paw elevation (Pain 1) during the second phase was also lower in CID16020046-treated rats but this effect did not reach statistical significance (Fig. 2B). Reference: Neuroscience. 2020 Sep 1;443:19-29. https://pubmed.ncbi.nlm.nih.gov/32673629/
Solvent mg/mL mM comments
Solubility
DMSO 63.1 148.41
DMF 25.0 58.76
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 425.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zeng Y, Liu Z, Tan X, Lei L. The GPR55 antagonist CID16020046 mitigates advanced glycation end products (AGEs)- induced chondrocyte activation. Chem Biol Interact. 2020 Jul 1;325:109088. doi: 10.1016/j.cbi.2020.109088. Epub 2020 May 1. PMID: 32360554. 2. Wang Y, Pan W, Wang Y, Yin Y. The GPR55 antagonist CID16020046 protects against ox-LDL-induced inflammation in human aortic endothelial cells (HAECs). Arch Biochem Biophys. 2020 Mar 15;681:108254. doi: 10.1016/j.abb.2020.108254. Epub 2020 Jan 3. PMID: 31904362. 3. Okine BN, Mc Laughlin G, Gaspar JC, Harhen B, Roche M, Finn DP. Antinociceptive Effects of the GPR55 Antagonist CID16020046 Injected into the Rat Anterior Cingulate Cortex. Neuroscience. 2020 Sep 1;443:19-29. doi: 10.1016/j.neuroscience.2020.07.013. Epub 2020 Jul 13. PMID: 32673629. 4. Montecucco F, Bondarenko AI, Lenglet S, Burger F, Piscitelli F, Carbone F, Roth A, Liberale L, Dallegri F, Brandt KJ, Fraga-Silva RA, Stergiopulos N, Di Marzo V, Mach F. Treatment with the GPR55 antagonist CID16020046 increases neutrophil activation in mouse atherogenesis. Thromb Haemost. 2016 Oct 28;116(5):987-997. doi: 10.1160/TH16-02-0139. Epub 2016 Jul 28. PMID: 27465665.
In vitro protocol:
1. Zeng Y, Liu Z, Tan X, Lei L. The GPR55 antagonist CID16020046 mitigates advanced glycation end products (AGEs)- induced chondrocyte activation. Chem Biol Interact. 2020 Jul 1;325:109088. doi: 10.1016/j.cbi.2020.109088. Epub 2020 May 1. PMID: 32360554. 2. Wang Y, Pan W, Wang Y, Yin Y. The GPR55 antagonist CID16020046 protects against ox-LDL-induced inflammation in human aortic endothelial cells (HAECs). Arch Biochem Biophys. 2020 Mar 15;681:108254. doi: 10.1016/j.abb.2020.108254. Epub 2020 Jan 3. PMID: 31904362.
In vivo protocol:
1. Okine BN, Mc Laughlin G, Gaspar JC, Harhen B, Roche M, Finn DP. Antinociceptive Effects of the GPR55 Antagonist CID16020046 Injected into the Rat Anterior Cingulate Cortex. Neuroscience. 2020 Sep 1;443:19-29. doi: 10.1016/j.neuroscience.2020.07.013. Epub 2020 Jul 13. PMID: 32673629. 2. Montecucco F, Bondarenko AI, Lenglet S, Burger F, Piscitelli F, Carbone F, Roth A, Liberale L, Dallegri F, Brandt KJ, Fraga-Silva RA, Stergiopulos N, Di Marzo V, Mach F. Treatment with the GPR55 antagonist CID16020046 increases neutrophil activation in mouse atherogenesis. Thromb Haemost. 2016 Oct 28;116(5):987-997. doi: 10.1160/TH16-02-0139. Epub 2016 Jul 28. PMID: 27465665.
1: López-Lariz CH, Marichal-Cancino BA. ML184 influences coping strategies via GPR55-dependent mechanisms following its delivery in the periaqueductal gray (PAG) region. Neuroscience. 2025 Jun 10:S0306-4522(25)00699-2. doi: 10.1016/j.neuroscience.2025.06.016. Epub ahead of print. PMID: 40506007. 2: Lee JE, Im DS. GPR55 Antagonist CID16020046 Suppresses Collagen-Induced Rheumatoid Arthritis by Suppressing Th1/Th17 Cells in Mice. Int J Mol Sci. 2025 May 14;26(10):4680. doi: 10.3390/ijms26104680. PMID: 40429822; PMCID: PMC12112631. 3: Lottero-Leconte R, Lara A, Plaza J, Arroyo-Salvo C, Bogetti ME, Rivolta AEY, Dellavalle F, Sengiali F, Cetica P, Rio S, Zalazar L, Cesari A, Miragaya M, Morado S, Perez-Martinez S. Role of GPR55 receptor in bovine sperm capacitation. Andrology. 2025 Jan 3. doi: 10.1111/andr.13823. Epub ahead of print. PMID: 39749764. 4: Son SE, Im DS. GPR55 antagonist CID16020046 suppresses DNCB-induced atopic dermatitis-like symptoms by suppressing Th1/Th2/Th17 populations in mice. Eur J Pharmacol. 2024 Dec 15;985:177088. doi: 10.1016/j.ejphar.2024.177088. Epub 2024 Oct 31. PMID: 39486767. 5: Schopohl B, Kohlhaas M, Nickel AG, Schiuma AF, Maas SL, van der Vorst EPC, Shia YX, Maack C, Steffens S, Puhl SL. Gpr55 deficiency crucially alters cardiomyocyte homeostasis and counteracts angiotensin II induced maladaption in female mice. Br J Pharmacol. 2025 Feb;182(3):670-691. doi: 10.1111/bph.17350. Epub 2024 Oct 20. PMID: 39428581. 6: Jiang W, Yu W, Tan Y. Activation of GPR55 alleviates neuropathic pain and chronic inflammation. Biotechnol Appl Biochem. 2025 Feb;72(1):196-206. doi: 10.1002/bab.2656. Epub 2024 Sep 1. PMID: 39219239. 7: Son SE, Lee YJ, Shin YJ, Kim DH, Im DS. GPR55 Antagonist CID16020046 Attenuates Obesity-Induced Airway Inflammation by Suppressing Chronic Low-Grade Inflammation in the Lungs. Int J Mol Sci. 2024 Jul 4;25(13):7358. doi: 10.3390/ijms25137358. PMID: 39000464; PMCID: PMC11242637. 8: Patricio F, Morales Dávila E, Patricio-Martínez A, Arana Del Carmen N, Martínez I, Aguilera J, Perez-Aguilar JM, Limón ID. Intrapallidal injection of cannabidiol or a selective GPR55 antagonist decreases motor asymmetry and improves fine motor skills in hemiparkinsonian rats. Front Pharmacol. 2022 Sep 2;13:945836. doi: 10.3389/fphar.2022.945836. PMID: 36120297; PMCID: PMC9479130. 9: Sánchez-Zavaleta R, Ávalos-Fuentes JA, González-Hernández AV, Recillas- Morales S, Paz-Bermúdez FJ, Leyva-Gómez G, Cortés H, Florán B. Presynaptic nigral GPR55 receptors stimulate [3 H]-GABA release through [3 H]-cAMP production and PKA activation and promote motor behavior. Synapse. 2022 Sep;76(11-12):e22246. doi: 10.1002/syn.22246. Epub 2022 Jul 23. PMID: 35831708. 10: Shen SY, Yu R, Li W, Liang LF, Han QQ, Huang HJ, Li B, Xu SF, Wu GC, Zhang YQ, Yu J. The neuroprotective effects of GPR55 against hippocampal neuroinflammation and impaired adult neurogenesis in CSDS mice. Neurobiol Dis. 2022 Jul;169:105743. doi: 10.1016/j.nbd.2022.105743. Epub 2022 Apr 28. PMID: 35490927. 11: Chen R, Xu H, Guo Z, Zhang P, Chen J, Chen Z. CID16020046, a GPR55 antagonist, attenuates sepsis‑induced acute kidney injury. Mol Med Rep. 2022 May;25(5):155. doi: 10.3892/mmr.2022.12671. Epub 2022 Mar 4. PMID: 35244189; PMCID: PMC8941374. 12: Zúñiga-Romero Á, Rivera-Plata Q, Arrieta J, Flores-Murrieta FJ, Rodríguez- Silverio J, Reyes-García JG, Huerta-Cruz JC, Ramírez-Martínez G, Rocha-González HI. GPR55 and GPR119 Receptors Contribute to the Processing of Neuropathic Pain in Rats. Pharmaceuticals (Basel). 2022 Jan 5;15(1):67. doi: 10.3390/ph15010067. PMID: 35056124; PMCID: PMC8778754. 13: Lee SJ, Im DS. GPR55 Antagonist CID16020046 Protects against Atherosclerosis Development in Mice by Inhibiting Monocyte Adhesion and Mac-1 Expression. Int J Mol Sci. 2021 Dec 3;22(23):13084. doi: 10.3390/ijms222313084. PMID: 34884889; PMCID: PMC8658038. 14: Kurano M, Kobayashi T, Sakai E, Tsukamoto K, Yatomi Y. Lysophosphatidylinositol, especially albumin-bound form, induces inflammatory cytokines in macrophages. FASEB J. 2021 Jun;35(6):e21673. doi: 10.1096/fj.202100245R. PMID: 34042213. 15: Kang S, Lee AY, Park SY, Liu KH, Im DS. O-1602 Promotes Hepatic Steatosis through GPR55 and PI3 Kinase/Akt/SREBP-1c Signaling in Mice. Int J Mol Sci. 2021 Mar 17;22(6):3091. doi: 10.3390/ijms22063091. PMID: 33803038; PMCID: PMC8003045. 16: Kolbe MR, Hohmann T, Hohmann U, Ghadban C, Mackie K, Zöller C, Prell J, Illert J, Strauss C, Dehghani F. THC Reduces Ki67-Immunoreactive Cells Derived from Human Primary Glioblastoma in a GPR55-Dependent Manner. Cancers (Basel). 2021 Mar 3;13(5):1064. doi: 10.3390/cancers13051064. PMID: 33802282; PMCID: PMC7959141. 17: Okine BN, Mc Laughlin G, Gaspar JC, Harhen B, Roche M, Finn DP. Antinociceptive Effects of the GPR55 Antagonist CID16020046 Injected into the Rat Anterior Cingulate Cortex. Neuroscience. 2020 Sep 1;443:19-29. doi: 10.1016/j.neuroscience.2020.07.013. Epub 2020 Jul 13. PMID: 32673629. 18: Minamihata T, Takano K, Moriyama M, Nakamura Y. Lysophosphatidylinositol, an Endogenous Ligand for G Protein-Coupled Receptor 55, Has Anti-inflammatory Effects in Cultured Microglia. Inflammation. 2020 Oct;43(5):1971-1987. doi: 10.1007/s10753-020-01271-4. PMID: 32519268. 19: Zeng Y, Liu Z, Tan X, Lei L. The GPR55 antagonist CID16020046 mitigates advanced glycation end products (AGEs)- induced chondrocyte activation. Chem Biol Interact. 2020 Jul 1;325:109088. doi: 10.1016/j.cbi.2020.109088. Epub 2020 May 1. PMID: 32360554. 20: Wang Y, Pan W, Wang Y, Yin Y. The GPR55 antagonist CID16020046 protects against ox-LDL-induced inflammation in human aortic endothelial cells (HAECs). Arch Biochem Biophys. 2020 Mar 15;681:108254. doi: 10.1016/j.abb.2020.108254. Epub 2020 Jan 3. PMID: 31904362.

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