CXCL12[1]

[1]. Steurer M, Montillo M, Scarfò L, Mauro FR, Andel J, Wildner S, Trentin L, Janssens A, Burgstaller S, Frömming A, Dümmler T, Riecke K, Baumann M, Beyer D, Vauléon S, Ghia P, Foà R, Caligaris-Cappio F, Gobbi M. Olaptesed pegol (NOX-A12) with bendamustine and rituximab: a phase IIa study in patients with relapsed/refractory chronic lymphocytic leukemia. Haematologica. 2019 Oct;104(10):2053-2060.

Olaptesed Pegol has been investigated for its use in the treatment of hematopoietic stem cell transplantation. Lexaptepid Pegol has been tested for its use in the treatment of anemia, inflammation, chronic disease, end-stage renal disease, and anemia due to chronic disease. Lexaptepid Pegol is a proprietary 44-nucleotide L-stereoisomeric RNA oligonucleotide conjugated with 40 kDa polyethylene glycol (PEG) that targets hepcidin and has potential anti-anemic activity. Following intravenous or subcutaneous injection, lexaptepid Pegol binds to hepcidin, preventing its binding to iron channel proteins located on the basolateral membrane of intestinal cells and the plasma membrane of macrophages in the gastrointestinal tract. This prevents hepcidin-induced internalization and degradation of iron channel proteins, thereby reducing iron retention in macrophages. The binding of NOX-H94 to hepcidin restores plasma iron levels to normal and promotes erythropoiesis. This may suppress inflammation-induced anemia. Hepcidin is a peptide hormone that plays a crucial role in maintaining systemic iron homeostasis. Its expression is upregulated by cytokines during acute and chronic inflammation. The drug's unique mirror-image conformation makes it resistant to hydrolysis and has low antigenicity. Pegylation prolongs its half-life. Olaptesed Pegol is a 45-mer L-stereoisomer RNA oligonucleotide linked to 40 kDa polyethylene glycol, targeting the small chemokine stromal cell-derived factor 1 (SDF-1 or CXCL12), and possesses potential anti-tumor and hematopoietic stem cell mobilization activities. NOX-A12, a drug targeting SDF-1, specifically binds to SDF-1, thereby preventing SDF-1 from binding to its receptors CXCR4 and CXCR7, and thus blocking receptor activation. This may inhibit angiogenesis, tumor cell proliferation, invasion, and metastasis, and enhance tumor cell sensitivity to chemotherapy. Furthermore, inhibition of the SDF-1/CXCR4 interaction may induce the mobilization of hematopoietic cells from the bone marrow into the bloodstream. The drug's unique mirror-image configuration makes it resistant to hydrolysis and it does not hybridize with natural nucleic acids. Furthermore, the drug does not induce an innate immune response and has shown good immunogenicity.

C18H37N2O10P

472.467547178268

472.218

1390628-22-4

Olaptesed pegol sodium

86278354

Typically exists as solid at room temperature

-1.8

3

10

21

31

518

0

QJAGBAPUFWBVSD-UHFFFAOYSA-N

InChI=1S/C18H37N2O10P/c1-26-11-13-28-10-8-20(18(22)16-29-14-12-27-2)15-17(21)19-7-5-3-4-6-9-30-31(23,24)25/h3-16H2,1-2H3,(H,19,21)(H2,23,24,25)

6-[[2-[[2-(2-methoxyethoxy)acetyl]-[2-(2-methoxyethoxy)ethyl]amino]acetyl]amino]hexyl dihydrogen phosphate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)