A4052-10g | Doxycycline hyclate [24390-14-5] Clinisciences

Doxycycline hyclate is an antibiotic [1].

Doxycycline hyclate is a derivative of tetracycline and possesses the activities of anti-inflammatory and antimicrobial. Doxycycline inhibits dengue virus replication in vitro with a temperature-dependent manner. The IC50 value is 52.3μM at 37°C and 26.7μM at 40°C. It inhibits the dengue virus via inhibiting the NS2B-NS3 serine protease of the virus. 60μM doxycycline reduces the CPE of the DNEV2-infected cells [1].

Doxycycline is found to be an inhibitor of MMP. Doxycycline treatment reduces MMP-8 and -9 levels and inhibits expression of tissue MMP-2 and MMP-9. Moreover, treatment with doxycycline significantly reduces the incidence of intracranial aneurysms. Doxycycline has also been reported to be an anti-inflammatory agent based on its inhibition of matrix metalloproteinases. In addition, doxycycline has potent antimalarial activity with IC50 value of 320nM at 96h in vitro [2, 3].

References:
[1] Rothan HA, Mohamed Z, Paydar M, Rahman NA, Yusof R. Inhibitory effect of doxycycline against dengue virus replication in vitro. Arch Virol. 2014 Apr;159(4):711-8.
[2] Maradni A, Khoshnevisan A, Mousavi SH, Emamirazavi SH, Noruzijavidan A. Role of matrix metalloproteinases (MMPs) and MMP inhibitors on intracranial aneurysms: a review article. Med J Islam Repub Iran. 2013 Nov;27(4):249-254.
[3] Draper MP, Bhatia B, Assefa H, Honeyman L, Garrity-Ryan LK, Verma AK, Gut J, Larson K, Donatelli J, Macone A, Klausner K, Leahy RG, Odinecs A, Ohemeng K, Rosenthal PJ, Nelson ML. In vitro and in vivo antimalarial efficacies of optimized tetracyclines. Antimicrob Agents Chemother. 2013 Jul;57(7):3131-6.

1. Yuting Li, Ziqiong Yang, et al. "Prdm14 promotes mouse ESC self-renewal and PGCLC specification through enhancement of Stat3 activity." iScience. 2022 Oct 6;25(11):105293. PMID: 36300005

Storage	Store at 4°C
M.Wt	512.94
Cas No.	24390-14-5
Formula	C₂₃H₂₉ClN₂O₉
Solubility	≥22.15 mg/mL in DMSO; insoluble in EtOH; ≥49.2 mg/mL in H2O with ultrasonic
SDF	Download SDF
Canonical SMILES	O=C(N)C(C1=O)=C([C@H]([C@@]2([C@H]([C@@]3([C@H](C4=C(C(O)=CC=C4)C(C3=C([C@@]21O)O)=O)C)20)O)20)N(C)C)O.Cl.[0.5H2O].[0.5C2H6O]
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Cell experiment [1]:
Cell lines	cultured P. falciparum parasites
Preparation method	The solubility of this compound in DMSO is >22.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	96-h
Applications	In cultured P. falciparum parasites, Doxycycline demonstrated nanomolar antimalarial activity with IC50 value of 330 nM.
Animal experiment [1]:
Animal models	mouse model of P. berghei malaria
Dosage form	10 mg/kg and 50 mg/kg once daily; dissolved in PBS in a total volume of 100 μl; intraperitoneally
Application	In mouse model of P. berghei malaria, Doxycycline exhibited potent antimalarial activity at 50 mg/kg and activity was suboptimal at 10 mg/kg.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1] Draper MP, Bhatia B, Assefa H, Honeyman L, Garrity-Ryan LK, Verma AK, Gut J, Larson K, Donatelli J, Macone A, Klausner K, Leahy RG, Odinecs A, Ohemeng K, Rosenthal PJ, Nelson ML. In vitro and in vivo antimalarial efficacies of optimized tetracyclines. Antimicrob Agents Chemother. 2013 Jul;57(7):3131-6.

Purity = 98.00%

Doxycycline hyclate [24390-14-5]

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