1. GPCR/G Protein
    Neuronal Signaling
  2. Somatostatin Receptor
  3. Pasireotide acetate

Pasireotide acetate (Synonyms: SOM230 acetate)

Cat. No.: HY-16381A Purity: 99.76%
Handling Instructions

Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate exhibits antisecretory, antiproliferative, and proapoptotic activity.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Pasireotide acetate Chemical Structure

Pasireotide acetate Chemical Structure

CAS No. : 396091-76-2

Size Price Stock Quantity
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 990 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1880 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2700 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate exhibits antisecretory, antiproliferative, and proapoptotic activity[1][2].

IC50 & Target

pKi: 8.2 (sst1), 9.0 (sst2), 9.1 (sst3), <7.0 (sst4), 9.9 (sst5)[1]

In Vitro

Pasireotide acetate exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively)[1].
Pasireotide acetate effectively inhibits the growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells, with an IC50 of 0.4 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pasireotide acetate (160 mg/kg/mouth; s.c. for 4 months) significantly decreases the serum insulin, increases serum glucose, reduces the tumor size and increases apoptosis in Pdx1-Cre[2].
Pasireotide acetate (2-50 μg/kg; s.c. twice daily for 42 days) exerts the antinociceptive and antiinflammatory actions via the SSTR2 receptor in a mouse model of immune-mediated arthritis[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 12 month-old conditional Men1 knockout mice with insulinoma[2]
Dosage: 160 mg/kg/mouth
Administration: S.c. every month for 4 months
Result: Decreased the serum insulin from 1.060 μg/L to 0.3653 μg/L and increased the serum glucose from 4.246 mM to 7.122 mM.
Significantly reduced the tumor size and increased apoptosis.
Molecular Weight

1107.26

Formula

C₆₀H₇₀N₁₀O₁₁

CAS No.
Sequence Shortening

Cyclo[{4-(NH2-C2H4-NH-CO-O-)Pro}-Phg-{D-Trp}-K-{Tyr(4-Bzl)}-F]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Protect from light, stored under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (90.31 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9031 mL 4.5157 mL 9.0313 mL
5 mM 0.1806 mL 0.9031 mL 1.8063 mL
10 mM 0.0903 mL 0.4516 mL 0.9031 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (2.26 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Pasireotide acetate
Cat. No.:
HY-16381A
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