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Chemical Structure| 191868-14-1 Chemical Structure| 191868-14-1

Structure of BIBO3304 TFA
CAS No.: 191868-14-1

Chemical Structure| 191868-14-1

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BIBO3304 TFA is a highly selective neuropeptide Y (NPY) Y1 receptor antagonist that effectively blocks its activity by binding to a specific site on the receptor. It shows potential in treating anxiety, depression, and related neurological disorders.

Synonyms: BIBO-3304(trifluoroacetate salt); BIBO 3304 Trifluoroacetate; BIBO3304

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Product Details of BIBO3304 TFA

CAS No. :191868-14-1
Formula : C31H36F3N7O5
M.W : 643.66
SMILES Code : OC(C(F)(F)F)=O.NC(NCC(C=C1)=CC=C1CNC([C@@H](CCCNC(N)=N)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O)=O
Synonyms :
BIBO-3304(trifluoroacetate salt); BIBO 3304 Trifluoroacetate; BIBO3304
MDL No. :MFCD04112989
InChI Key :FBMCYYWIBYEOST-GJFSDDNBSA-N
Pubchem ID :5311021

Safety of BIBO3304 TFA

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse islet cells 1 μM 72 h reduced cytokine-induced apoptosis Mol Metab. 2022 Jan;55:101413
mouse islet cells 1 μM 24 h restored glucose-stimulated insulin secretion under ER stress conditions Mol Metab. 2022 Jan;55:101413
mouse islet cells 1 μM 18 h reduced oxidative stress-induced apoptosis Mol Metab. 2022 Jan;55:101413
vascular smooth muscle cells 1 μM blocked NPY-induced vasoconstriction Eur Heart J. 2019 Jun 21;40(24):1920-1929
db/db mouse islet cells 1 μM 36 h reduced apoptotic gene expression and increased pCREB levels Mol Metab. 2022 Jan;55:101413
KPR172HC cells 1 μM 8 h To evaluate the effect of BIBO3304 on the migratory capacity of KPR172HC cells, results showed that BIBO3304 significantly reduced the migratory capacity of KPR172HC cells. Sci Adv. 2025 Mar 14;11(11):eadq4416
mouse islet cells 1 μM 48 h restored glucose-stimulated insulin secretion under inflammatory conditions Mol Metab. 2022 Jan;55:101413
human pulmonary arterial smooth muscle cells (hPASMC) 1 μM 3 min Used to block Y1 receptors to study their role in NPY-induced intracellular calcium increase. The results showed that BIBO 3304 significantly inhibited NPY-induced calcium influx Br J Pharmacol. 2014 Aug;171(16):3895-907
rabbit pulmonary artery smooth muscle cells 1 nM 60 min To investigate the effect of BIBO3304 on the electrically-evoked biphasic contraction of rabbit intrapulmonary artery, results showed no significant effect of BIBO3304 on the contraction. Br J Pharmacol. 2002 Oct;137(4):488-96

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice High-fat diet-induced obesity model Oral jelly 1 mg/mL Once daily for 7 weeks Selective antagonism of peripheral Y1R leads to a significant reduction in body weight gain, reduced fat mass, increased energy expenditure, enhanced thermogenesis in brown adipose tissue (BAT), and extensive browning of white adipose tissue (WAT) Nat Commun. 2021 May 11;12(1):2622
Mice KPR172HC pancreatic cancer model Intraperitoneal injection 1 mg/kg Once daily for 12 days To evaluate the effect of BIBO3304 on liver metastasis of pancreatic cancer, results showed that BIBO3304 significantly reduced liver metastatic burden. Sci Adv. 2025 Mar 14;11(11):eadq4416
Mice Y2 receptor knockout and wild-type mice Intravenous injection 0.5 µmol/kg Single dose, observed for 30 minutes BIBO3304 blocked responses to the Y1 agonist at lower doses but only partially inhibited at higher doses in Y2+/+ mice. In Y2 knockout mice, responses to the Y2 agonist were abolished at lower doses and partially reduced at the highest dose tested, while responses to the Y1 agonist were similar in both Y2+/+ and Y2 knockout mice. Br J Pharmacol. 2003 Sep;140(2):422-30
Rats Rat PVN injection model PVN injection 30 μg Single dose Evaluate the inhibitory effect of BIBO3304 on NPY-induced feeding behavior Br J Pharmacol. 1998 Oct;125(3):549-55

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.55mL

0.31mL

0.16mL

7.77mL

1.55mL

0.78mL

15.54mL

3.11mL

1.55mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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